New pollutant pharmaceutical and personal care products(PPCPs),especially antiviral drugs,have received increasing attention not only due to their increase in usage after the outbreak of COVID-19 epidemics but also du...New pollutant pharmaceutical and personal care products(PPCPs),especially antiviral drugs,have received increasing attention not only due to their increase in usage after the outbreak of COVID-19 epidemics but also due to their adverse impacts on water ecological environment.Electro-Fenton technology is an effective method to remove PPCPs from water.Novel particle electrodes(MMT/rGO/Fe_(3)O_(4))were synthesized by depositing Fe3O4 nanoparticles on reduced graphene oxide modified montmorillonite and acted as catalysts to promote oxidation performance in a three-dimensional electro-Fenton(3D-EF)system.The electrodes combined the catalytic property of Fe3O4,hydrophilicity of montmorillonite and electrical conductivity of graphene oxides,and applied for the degradation of Acyclovir(ACV)with high efficiency and ease of operation.At optimal condition,the degradation rate of ACV reached 100%within 120 min,and the applicable pH range could be 3 to 11 in the 3D-EF system.The stability and reusability of MMT/rGO/Fe_(3)O_(4)particle electrodes were also studied,the removal rate of ACV remained at 92%after 10 cycles,which was just slightly lower than that of the first cycle.Potential degradation mechanisms were also proposed by methanol quenching tests and FT-ICR-MS.展开更多
Herpes simplex virus type I is a cutaneous infection treated with acyclovir. The topical treatment has therapeutic challenges due to the deficient delivery of the drug through epithelial barriers. This results in an i...Herpes simplex virus type I is a cutaneous infection treated with acyclovir. The topical treatment has therapeutic challenges due to the deficient delivery of the drug through epithelial barriers. This results in an inadequate drug-virus interaction in the basal epidermis (virus replication site). For this reason, it is essential to generate drug carrier systems that overcome these limitations. In this study, we evaluated the permeation (through in vitro test Franz cells) and penetration (by ex vivo test Tape Stripping) of a topical formulation of acyclovir loaded in solid lipid nanoparticles and a conventional formulation (Aciclor®). The acyclovir solid lipid nanoparticles were prepared using hot homogenization and sonication methods. The results yielded a particle size of 85 ± 2 nm, a polydispersity index of 0.24 ± 0.01, a zeta potential of −16 ± 2 mV, and 94% ± 3% of encapsulated drug. The in vitro test revealed that the permeability of acyclovir solid lipid nanoparticles formulation was superior compared to reference formulation, with values of 1473.74 ± 30.14 µg/cm2 for the solid lipid nanoparticles and 893.36 ± 38.09 µg/cm2 for the reference formulation. The ex vivo test demonstrated that acyclovir solid lipid nanoparticles exhibited superior penetrability through the stratum corneum compared to the reference formulation, with total amounts of 3767 µg for the solid lipid nanoparticles and 2162 µg for the reference formulation. These findings seem promising in advancing new effective therapies against herpes generated by herpes simplex virus type I.展开更多
Objective To establish a rapid,sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of acyclovir (the metabolite of valacyclovir hydrochloride) in human plasma...Objective To establish a rapid,sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of acyclovir (the metabolite of valacyclovir hydrochloride) in human plasma. Methods After addition of ganciclovir as internal standard (IS),plasma samples were prepared by one-step protein precipitation using acetonitrile as precipitant,followed by an isocratic elution with 0.1% formic acid solution-methanol (95∶5,v/v) on an Agilent ZORBAX SB-C18 (150mm×2.1mm i.d.,3.5μm) column. Detection was performed on a triple-quadrupole mass spectrometer utilizing electrospray ionization (ESI) interface operating in positive ion and selected reaction monitoring (SRM) mode with the precursor to product ion transitions m/z 226.2→152.1 for acyclovir and m/z 256.2→152.1 for the IS. Results The analytical results demonstrated a good linearity over the ranges from 0.005 to 4μg/mL (r=0.9999) for valacyclovir hydrochloride. The relative standard deviations (RSD) of intra-batch and inter-batch were less than 4.06% and 9.23%,respectively. The limit of detection and lower limit of quantification in human plasma were 2ng/mL and 5ng/mL,respectively. Conclusion The method was simple,sensitive,accurate and reproducible and has been successfully applied to a bioequivalence study of valacyclovir hydrochloride capsules in Chinese healthy male volunteers.展开更多
BACKGROUND： The study aimed to investigate the clinical characteristics of acute renal failure（ARF） caused by oral acyclovir.METHODS： A 45-year-old Chinese male patient with acyclovir-induced ARF suffered fromabdo...BACKGROUND： The study aimed to investigate the clinical characteristics of acute renal failure（ARF） caused by oral acyclovir.METHODS： A 45-year-old Chinese male patient with acyclovir-induced ARF suffered fromabdominal pain for one day. The pain was extended to the epigastric area from the right lowerquadrant. Transient oliguria was seen in addition to microscopic hematuria and proteinuria. Theserum creatinine concentration was 304 !mol/L. Eight days before the occurrence of ARF, the patienttook oral acyclovir for facial neuritis.RESULTS： His renal function was restored completely following the discontinuation of acyclovir,with continuous renal replacement therapy for 54 hours and some symptomatic treatment.CONCLUSION： The presentation of acute renal failure caused by acyclovir can be diverse, butthe prognosis is good after active treatment.展开更多
The synthesis of acyclovir and L-ascorbic acid with divinyladipate was performed with alkaline protease from Bacillus subtilis and lipase from Lipozyme (immobilized from Mucor miehei) in different anhydrous organic so...The synthesis of acyclovir and L-ascorbic acid with divinyladipate was performed with alkaline protease from Bacillus subtilis and lipase from Lipozyme (immobilized from Mucor miehei) in different anhydrous organic solvents. Two corresponding derivatives were obtained.展开更多
Objective:To formulate and evaluate acyclovir microcapsules using bakers yeast.Methods: Acyclovir,pretreated yeast and deionised water were taken at a volumetric ratio of 1:2:4 respectively.This suspension was agitate...Objective:To formulate and evaluate acyclovir microcapsules using bakers yeast.Methods: Acyclovir,pretreated yeast and deionised water were taken at a volumetric ratio of 1:2:4 respectively.This suspension was agitated in a magnetic stirrer at 25℃30℃.35℃,and 40℃for 4 hours.The suspension was then centrifuged for 10 minutes at 2 000 rpm.The supernatant solution was decanted and the cells were washed 5 times with deionised water.Then the suspended drug entrapped yeast cells were dried in a lyophillizer for 48 hours.The yield was noted.Results:The first four formulations were done with 200 mg of the drug,followed by 400 mg for the next four formulations and 800 mg the last four formulations.SEM showed that the surface of the microcapsules was intact,with no burst characteristics.FTIR showed no interaction between acyclovir and the cell wall.DSC showed that the peak was within the standard values. The mean particle size for all the samples was 8μm in diameter.The dissolution studies were done for all the twelve samples and showed a Fickian model of diffusion.Conclusions: From the results it is inferred that the samples prepared at 40℃(FY-4,FY- 8,FY-12) show better entrapment and release.So these samples are formulated in the form of a suspension and compared with marketed acyclovir suspension using HPLC technique.The formulated suspensions with FY-4,FY-8 and FY-12 shows drug content in accordance with the standards of the pharmacopoeial limits.展开更多
A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the des...A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.展开更多
A retroviral vector(LNHcTL)containing the herpes simplex virus type 1 thymldine kinase(HSVI-tk)gene was constructed and used for transduction of the gene into human hepatocellular carcinoma cells(SMMC-7721).Xenografte...A retroviral vector(LNHcTL)containing the herpes simplex virus type 1 thymldine kinase(HSVI-tk)gene was constructed and used for transduction of the gene into human hepatocellular carcinoma cells(SMMC-7721).Xenografted tumor on nude mice was produced with the injection of the transduced cells(SMMC- 7721/LN HcTL) inoculated subcutaneously and showed regression when treated with Acyclovir.The mean weight of the residual tumors was six times less than that of the controls'tumors. Patients with liver carcinoma were given an intratumoral injection of ampbotropic packing cells(PA317/LNHcTL)producing HSV1-tk recombinant retroviral particles,and then treated with Acyclovir intravenously, which showed a marked regression of the tumor.Our preliminary data suggest that HSV1-tk gene/Acyclovir system might be a useful therapeutic approach for the treatment of hepatic carcinoma in humans.展开更多
Risk assessment and uncertainty approximation are two major and important parameters that need to be adopted for the development of pharmaceutical process to ensure reliable results.Additionally,there is a need to swi...Risk assessment and uncertainty approximation are two major and important parameters that need to be adopted for the development of pharmaceutical process to ensure reliable results.Additionally,there is a need to switch from the traditional method validation checklist to provide a high level of assurance of method reliability to measure quality attribute of a drug product.In the present work,evaluation of risk profile,combined standard uncertainty and expanded uncertainty in the analysis of acyclovir were studied.Uncertainty was calculated using cause-effect approach,and to make it more accurately applicable a method was validated in our laboratory as per the ICH guidelines.While assessing the results of validation,the calibration model was justified by the lack of fit and Levene＇s test.Risk profile represents the future applications of this method.In uncertainty the major contribution is due to sample concentration and mass.This work demonstrates the application of theoretical concepts of calibration model tests,relative bias,risk profile and uncertainty in routine methods used for analysis in pharmaceutical field.展开更多
·AIM: To investigate the permeability of amniotic membrane in herpes virus cell culture to acyclovir with real time polymerase chain reaction(RT-PCR).·METHODS: Madin-Darby Bovine Kidney(MDBK) cell culture an...·AIM: To investigate the permeability of amniotic membrane in herpes virus cell culture to acyclovir with real time polymerase chain reaction(RT-PCR).·METHODS: Madin-Darby Bovine Kidney(MDBK) cell culture and Bovine Herpes Virus(BHV1) type 1 were used in the study. Cell cultures were grouped into two on the basis of herpes virus inoculation. Each group was sub-grouped into three. Amniotic membrane(V-HAM),acyclovir(V-A), and amniotic membrane and acyclovir(V-HAM-A) were applied to these subgroup cultures,respectively. After the application of the membrane and the drug, the cultures were evaluated at 24 and 48 h for cytopathic effect positive(CPE +) with a tissue culture microscope. In the CPE(+) samples, the DNA was extracted for viral DNA analysis by RT-PCR.·RESULTS: In control cultures without herpes virus CPE was not detected. Besides, amniotic membrane and acyclovir did not have cytotoxic effect on cell cultures.CPE were detected in Bovine Herpesvirus type-1inoculated cell cultures after amniotic membrane and/or acyclovir application. DNA analysis with RT-PCR indicated that Cycle threshold(Ct) values were lower in the BHV1 and membrane applied group(amniotic membrane group 【 acyclovir group 【 membrane and acyclovir group). This showed that membrane did not have antiviral effect. The membrane and acyclovir cell culture groups with high Ct values indicated thatmembrane was permeable and had a low barrier effect to drug.·CONCLUSION: In our in-vitro study, we found that amniotic membrane, which can be used in the treatment of corneal diseases, did not have antiviral effect. Besides,we detected that amniotic membrane was permeable to acyclovir in BHV-1 inoculated MDBK cell culture.However, more studies are necessary to investigate the quantitative effects of amniotic membrane and acyclovir.展开更多
The assay of acyclovir in plasma seems to be a challenge because of its high hydrophily.In our present study,a reversed-phase high-performance liquid chromatography(RP-HPLC)method for the determination of acyclovir in...The assay of acyclovir in plasma seems to be a challenge because of its high hydrophily.In our present study,a reversed-phase high-performance liquid chromatography(RP-HPLC)method for the determination of acyclovir in rat plasma was described and validated in drug-drug interaction(DDI)between gefitinib and acyclovir in rats.The analytes were separated with gradient elution on C18 column(4.6 mm×250 mm,5μm),and the peaks were recorded using ultraviolet detector at a wavelength of 254 nm.Protein precipitation followed by methyl tertiary butyl ether extraction was used for sample preparation.The calibration curve was established between 0.2 and 40μg/mL(r^(2)=0.9999).The intra-and inter-day precisions were all less than 8%,and all the biases were not more than 10%.This new method was successfully applied to a DDI study between gefitinib and acyclovir in rats.Gefitinib up-regulated the absorption of acyclovir by about three times,and our findings guided the clinical co-administration of epidermal growth factor receptor-tyrosine kinase inhibitors(EGFR-TKIs)with acyclovir.展开更多
Objective: To observe the effect of anciclovir (ACV) treatment on tumors induced by inoculation of TK gene-transfected human pulmonary adenocarcinoma A549 cells in nude mice. Methods: A recombinant plasmid containing ...Objective: To observe the effect of anciclovir (ACV) treatment on tumors induced by inoculation of TK gene-transfected human pulmonary adenocarcinoma A549 cells in nude mice. Methods: A recombinant plasmid containing TK gene was constructed and transfected into A549 cells by electroporation. The sensitivity of the transgenic cells (A549-TK) to ACV was examined by MTT assay in vitro and for in vivo observation, inoculation of A549-TK and A-549 cells into nude mice was separately performed to induce tumor growth, the response of which to ACV treatment was observed, and the tumor tissues were pathologically examined. Results: A recombinant plasmid containing TK gene was successfully constructed and transfected into A549 cells. The sensitivity of A549-TK cells to ACV was 43 times higher than that of A549 cells. The tumors induced by A549-TK cells showed no significant increase in size after ACV treatment (P>0. 05) , and light microscopy revealed local tissue necrosis, karyoklasis, and nuclei disappearance. Conclusion: A549-TK cells acquires sensitivity to ACV both in vitro and in vivo, and ACV can inhibit the growth of tumors induced by A549-TK cell inoculation in nude mice.展开更多
<strong>Background:</strong> Cytomegalovirus (CMV) is an important infection in renal transplant recipients and may significantly impact recipients’ long-term outcome and graft survival. <strong>Obj...<strong>Background:</strong> Cytomegalovirus (CMV) is an important infection in renal transplant recipients and may significantly impact recipients’ long-term outcome and graft survival. <strong>Objective:</strong> This study aimed to evaluate the benefit of prophylaxis with acyclovir on post-transplant CMV infection prevention in a population of renal transplant recipients in Lagos, Nigeria. <strong>Subjects and Methods:</strong> The study was a cross-sectional design involving renal transplant recipients attending post-transplant follow-up clinics in Lagos, Nigeria between October 2004 and July 2005. Data on the use of CMV prophylaxis were obtained from the hospital case records of the study subjects. Enzyme-Linked Immunosorbent Assay (ELISA) was employed to detect CMV IgM antibodies for the diagnosis of post-transplant CMV infection and Microsoft Excel and EPI-Info 2002 statistical software were used for data entry and analysis. <strong>Results:</strong> Forty (40) renal transplant recipients were studied, 32 recipients were males and 8 were females with M:F ratio of 4:1. The mean age of the recipients was 39 ± 11.6 years old. The recipients’ post-transplant duration ranged from 2 to 80 months (Mean 17.6 ± 18.6 months). Fifteen (37.5%) of the transplant recipients received acyclovir prophylaxis for six months, one recipient (2.5%) received ganciclovir prophylaxis for three weeks while 24 recipients (60%) received no prophylactic therapy. There was no significant difference in the prevalence of seropositive CMV-IgM between transplant recipients who used CMV prophylaxis and those who did not (Fisher exact p = 0.45). <strong>Conclusion:</strong> Prophylaxis with acyclovir for six months showed no significant benefit on post-transplant CMV infection prevention in renal transplant recipients.展开更多
This paper aimed at developing a simple and fast approach using chemometrics processing for direct assay of acyclovir in tablets by NIR （near infrared） spectroscopy in diffuse reflectance mode. In making trials with...This paper aimed at developing a simple and fast approach using chemometrics processing for direct assay of acyclovir in tablets by NIR （near infrared） spectroscopy in diffuse reflectance mode. In making trials with 5 different tablet matrices, the experimental results showed that regardless the matrix variation, it was always possible to construct a quantitative model with suitable linear range, accuracy and precision for direct assay of acyclovir in tablet from NIR spectra. Therefore, the approach used in this study was suitable for on-site fast assay of APIs in tablets during manufacturing process or in post-marketing surveillance of drug quality.展开更多
Graphene oxide(GO)and mesoporous silica nanoparticle(MSN)have been documented as advanced nanocarriers for drug delivery due to their unique and versatile properties.The design of GO-MSN nanocomposite offers a large s...Graphene oxide(GO)and mesoporous silica nanoparticle(MSN)have been documented as advanced nanocarriers for drug delivery due to their unique and versatile properties.The design of GO-MSN nanocomposite offers a large surface area,adjustable pore size,biocompatibility,and low cytotoxicity.The application of acyclovir(ACV)(BCS:III)is suffering from poor permeability,low bioavailability,etc.Hence,the use of GO-MSN nanocomposite for the delivery of ACV may overcome the limitations of ACV.Therefore,the present work aims to design the lipid-coated ACV-loaded GO-MSN(LC-ACV-GO-MSN)nanocomposites.In brief,the design of experiments(DoE,32 response surface methodology)approach was preferred for the development of GO-MSN nanocomposite.The loading of ACV in nanocomposite was done passive loading whereas the coating of lipids was done using a modified thin film hydration technique.At last,different spectral characterizations were performed.The output demonstrated that the entrapment efficiency of ACV-MSN and ACV-GO-MSN was 51.13%and 71.86%,respectively.Afterward,the designed LC-ACV-GO-MSN and ACV-GO-MSN nanocomposite shows 93.40%and 80.74%in vitro drug release,respectively.In conclusion,the design of LC-ACV-GO-MSN nanocomposite using optimized GO-MSN followed lipid coating offers the modified release.Therefore,in the future,LC-ACV-GO-MSN nanocomposite can be used for the delivery of ACV and other drug molecules with a high payload and enhanced release profile.We hope the current proof of concept may provide advantages over existing methods and emphasize the significance of protocells in cargo delivery systems.展开更多
基金the GDAS’Project of Science and Technology Development(No.2020GDASYL-20200103044)Key-Area Research and Development Program of Guangdong(No.2020B1111350002)+1 种基金the National Key R&D Program of China(No.2019YFC1805305)the Project of Water Resource Department of Guangdong Province(No.2017-18).
文摘New pollutant pharmaceutical and personal care products(PPCPs),especially antiviral drugs,have received increasing attention not only due to their increase in usage after the outbreak of COVID-19 epidemics but also due to their adverse impacts on water ecological environment.Electro-Fenton technology is an effective method to remove PPCPs from water.Novel particle electrodes(MMT/rGO/Fe_(3)O_(4))were synthesized by depositing Fe3O4 nanoparticles on reduced graphene oxide modified montmorillonite and acted as catalysts to promote oxidation performance in a three-dimensional electro-Fenton(3D-EF)system.The electrodes combined the catalytic property of Fe3O4,hydrophilicity of montmorillonite and electrical conductivity of graphene oxides,and applied for the degradation of Acyclovir(ACV)with high efficiency and ease of operation.At optimal condition,the degradation rate of ACV reached 100%within 120 min,and the applicable pH range could be 3 to 11 in the 3D-EF system.The stability and reusability of MMT/rGO/Fe_(3)O_(4)particle electrodes were also studied,the removal rate of ACV remained at 92%after 10 cycles,which was just slightly lower than that of the first cycle.Potential degradation mechanisms were also proposed by methanol quenching tests and FT-ICR-MS.
文摘Herpes simplex virus type I is a cutaneous infection treated with acyclovir. The topical treatment has therapeutic challenges due to the deficient delivery of the drug through epithelial barriers. This results in an inadequate drug-virus interaction in the basal epidermis (virus replication site). For this reason, it is essential to generate drug carrier systems that overcome these limitations. In this study, we evaluated the permeation (through in vitro test Franz cells) and penetration (by ex vivo test Tape Stripping) of a topical formulation of acyclovir loaded in solid lipid nanoparticles and a conventional formulation (Aciclor®). The acyclovir solid lipid nanoparticles were prepared using hot homogenization and sonication methods. The results yielded a particle size of 85 ± 2 nm, a polydispersity index of 0.24 ± 0.01, a zeta potential of −16 ± 2 mV, and 94% ± 3% of encapsulated drug. The in vitro test revealed that the permeability of acyclovir solid lipid nanoparticles formulation was superior compared to reference formulation, with values of 1473.74 ± 30.14 µg/cm2 for the solid lipid nanoparticles and 893.36 ± 38.09 µg/cm2 for the reference formulation. The ex vivo test demonstrated that acyclovir solid lipid nanoparticles exhibited superior penetrability through the stratum corneum compared to the reference formulation, with total amounts of 3767 µg for the solid lipid nanoparticles and 2162 µg for the reference formulation. These findings seem promising in advancing new effective therapies against herpes generated by herpes simplex virus type I.
文摘Objective To establish a rapid,sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of acyclovir (the metabolite of valacyclovir hydrochloride) in human plasma. Methods After addition of ganciclovir as internal standard (IS),plasma samples were prepared by one-step protein precipitation using acetonitrile as precipitant,followed by an isocratic elution with 0.1% formic acid solution-methanol (95∶5,v/v) on an Agilent ZORBAX SB-C18 (150mm×2.1mm i.d.,3.5μm) column. Detection was performed on a triple-quadrupole mass spectrometer utilizing electrospray ionization (ESI) interface operating in positive ion and selected reaction monitoring (SRM) mode with the precursor to product ion transitions m/z 226.2→152.1 for acyclovir and m/z 256.2→152.1 for the IS. Results The analytical results demonstrated a good linearity over the ranges from 0.005 to 4μg/mL (r=0.9999) for valacyclovir hydrochloride. The relative standard deviations (RSD) of intra-batch and inter-batch were less than 4.06% and 9.23%,respectively. The limit of detection and lower limit of quantification in human plasma were 2ng/mL and 5ng/mL,respectively. Conclusion The method was simple,sensitive,accurate and reproducible and has been successfully applied to a bioequivalence study of valacyclovir hydrochloride capsules in Chinese healthy male volunteers.
文摘BACKGROUND： The study aimed to investigate the clinical characteristics of acute renal failure（ARF） caused by oral acyclovir.METHODS： A 45-year-old Chinese male patient with acyclovir-induced ARF suffered fromabdominal pain for one day. The pain was extended to the epigastric area from the right lowerquadrant. Transient oliguria was seen in addition to microscopic hematuria and proteinuria. Theserum creatinine concentration was 304 !mol/L. Eight days before the occurrence of ARF, the patienttook oral acyclovir for facial neuritis.RESULTS： His renal function was restored completely following the discontinuation of acyclovir,with continuous renal replacement therapy for 54 hours and some symptomatic treatment.CONCLUSION： The presentation of acute renal failure caused by acyclovir can be diverse, butthe prognosis is good after active treatment.
文摘The synthesis of acyclovir and L-ascorbic acid with divinyladipate was performed with alkaline protease from Bacillus subtilis and lipase from Lipozyme (immobilized from Mucor miehei) in different anhydrous organic solvents. Two corresponding derivatives were obtained.
文摘Objective:To formulate and evaluate acyclovir microcapsules using bakers yeast.Methods: Acyclovir,pretreated yeast and deionised water were taken at a volumetric ratio of 1:2:4 respectively.This suspension was agitated in a magnetic stirrer at 25℃30℃.35℃,and 40℃for 4 hours.The suspension was then centrifuged for 10 minutes at 2 000 rpm.The supernatant solution was decanted and the cells were washed 5 times with deionised water.Then the suspended drug entrapped yeast cells were dried in a lyophillizer for 48 hours.The yield was noted.Results:The first four formulations were done with 200 mg of the drug,followed by 400 mg for the next four formulations and 800 mg the last four formulations.SEM showed that the surface of the microcapsules was intact,with no burst characteristics.FTIR showed no interaction between acyclovir and the cell wall.DSC showed that the peak was within the standard values. The mean particle size for all the samples was 8μm in diameter.The dissolution studies were done for all the twelve samples and showed a Fickian model of diffusion.Conclusions: From the results it is inferred that the samples prepared at 40℃(FY-4,FY- 8,FY-12) show better entrapment and release.So these samples are formulated in the form of a suspension and compared with marketed acyclovir suspension using HPLC technique.The formulated suspensions with FY-4,FY-8 and FY-12 shows drug content in accordance with the standards of the pharmacopoeial limits.
文摘A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.
文摘A retroviral vector(LNHcTL)containing the herpes simplex virus type 1 thymldine kinase(HSVI-tk)gene was constructed and used for transduction of the gene into human hepatocellular carcinoma cells(SMMC-7721).Xenografted tumor on nude mice was produced with the injection of the transduced cells(SMMC- 7721/LN HcTL) inoculated subcutaneously and showed regression when treated with Acyclovir.The mean weight of the residual tumors was six times less than that of the controls'tumors. Patients with liver carcinoma were given an intratumoral injection of ampbotropic packing cells(PA317/LNHcTL)producing HSV1-tk recombinant retroviral particles,and then treated with Acyclovir intravenously, which showed a marked regression of the tumor.Our preliminary data suggest that HSV1-tk gene/Acyclovir system might be a useful therapeutic approach for the treatment of hepatic carcinoma in humans.
文摘Risk assessment and uncertainty approximation are two major and important parameters that need to be adopted for the development of pharmaceutical process to ensure reliable results.Additionally,there is a need to switch from the traditional method validation checklist to provide a high level of assurance of method reliability to measure quality attribute of a drug product.In the present work,evaluation of risk profile,combined standard uncertainty and expanded uncertainty in the analysis of acyclovir were studied.Uncertainty was calculated using cause-effect approach,and to make it more accurately applicable a method was validated in our laboratory as per the ICH guidelines.While assessing the results of validation,the calibration model was justified by the lack of fit and Levene＇s test.Risk profile represents the future applications of this method.In uncertainty the major contribution is due to sample concentration and mass.This work demonstrates the application of theoretical concepts of calibration model tests,relative bias,risk profile and uncertainty in routine methods used for analysis in pharmaceutical field.
文摘·AIM: To investigate the permeability of amniotic membrane in herpes virus cell culture to acyclovir with real time polymerase chain reaction(RT-PCR).·METHODS: Madin-Darby Bovine Kidney(MDBK) cell culture and Bovine Herpes Virus(BHV1) type 1 were used in the study. Cell cultures were grouped into two on the basis of herpes virus inoculation. Each group was sub-grouped into three. Amniotic membrane(V-HAM),acyclovir(V-A), and amniotic membrane and acyclovir(V-HAM-A) were applied to these subgroup cultures,respectively. After the application of the membrane and the drug, the cultures were evaluated at 24 and 48 h for cytopathic effect positive(CPE +) with a tissue culture microscope. In the CPE(+) samples, the DNA was extracted for viral DNA analysis by RT-PCR.·RESULTS: In control cultures without herpes virus CPE was not detected. Besides, amniotic membrane and acyclovir did not have cytotoxic effect on cell cultures.CPE were detected in Bovine Herpesvirus type-1inoculated cell cultures after amniotic membrane and/or acyclovir application. DNA analysis with RT-PCR indicated that Cycle threshold(Ct) values were lower in the BHV1 and membrane applied group(amniotic membrane group 【 acyclovir group 【 membrane and acyclovir group). This showed that membrane did not have antiviral effect. The membrane and acyclovir cell culture groups with high Ct values indicated thatmembrane was permeable and had a low barrier effect to drug.·CONCLUSION: In our in-vitro study, we found that amniotic membrane, which can be used in the treatment of corneal diseases, did not have antiviral effect. Besides,we detected that amniotic membrane was permeable to acyclovir in BHV-1 inoculated MDBK cell culture.However, more studies are necessary to investigate the quantitative effects of amniotic membrane and acyclovir.
基金Discipline and Master's Site Construction Project of Guiyang University by Guiyang City Financial Support Guiyang University (Grant No. SY-2020)Guizhou Biopharmaceutical Engineering Research Center (Grant No. QJH KYZ[2019]051)。
文摘The assay of acyclovir in plasma seems to be a challenge because of its high hydrophily.In our present study,a reversed-phase high-performance liquid chromatography(RP-HPLC)method for the determination of acyclovir in rat plasma was described and validated in drug-drug interaction(DDI)between gefitinib and acyclovir in rats.The analytes were separated with gradient elution on C18 column(4.6 mm×250 mm,5μm),and the peaks were recorded using ultraviolet detector at a wavelength of 254 nm.Protein precipitation followed by methyl tertiary butyl ether extraction was used for sample preparation.The calibration curve was established between 0.2 and 40μg/mL(r^(2)=0.9999).The intra-and inter-day precisions were all less than 8%,and all the biases were not more than 10%.This new method was successfully applied to a DDI study between gefitinib and acyclovir in rats.Gefitinib up-regulated the absorption of acyclovir by about three times,and our findings guided the clinical co-administration of epidermal growth factor receptor-tyrosine kinase inhibitors(EGFR-TKIs)with acyclovir.
文摘Objective: To observe the effect of anciclovir (ACV) treatment on tumors induced by inoculation of TK gene-transfected human pulmonary adenocarcinoma A549 cells in nude mice. Methods: A recombinant plasmid containing TK gene was constructed and transfected into A549 cells by electroporation. The sensitivity of the transgenic cells (A549-TK) to ACV was examined by MTT assay in vitro and for in vivo observation, inoculation of A549-TK and A-549 cells into nude mice was separately performed to induce tumor growth, the response of which to ACV treatment was observed, and the tumor tissues were pathologically examined. Results: A recombinant plasmid containing TK gene was successfully constructed and transfected into A549 cells. The sensitivity of A549-TK cells to ACV was 43 times higher than that of A549 cells. The tumors induced by A549-TK cells showed no significant increase in size after ACV treatment (P>0. 05) , and light microscopy revealed local tissue necrosis, karyoklasis, and nuclei disappearance. Conclusion: A549-TK cells acquires sensitivity to ACV both in vitro and in vivo, and ACV can inhibit the growth of tumors induced by A549-TK cell inoculation in nude mice.
文摘<strong>Background:</strong> Cytomegalovirus (CMV) is an important infection in renal transplant recipients and may significantly impact recipients’ long-term outcome and graft survival. <strong>Objective:</strong> This study aimed to evaluate the benefit of prophylaxis with acyclovir on post-transplant CMV infection prevention in a population of renal transplant recipients in Lagos, Nigeria. <strong>Subjects and Methods:</strong> The study was a cross-sectional design involving renal transplant recipients attending post-transplant follow-up clinics in Lagos, Nigeria between October 2004 and July 2005. Data on the use of CMV prophylaxis were obtained from the hospital case records of the study subjects. Enzyme-Linked Immunosorbent Assay (ELISA) was employed to detect CMV IgM antibodies for the diagnosis of post-transplant CMV infection and Microsoft Excel and EPI-Info 2002 statistical software were used for data entry and analysis. <strong>Results:</strong> Forty (40) renal transplant recipients were studied, 32 recipients were males and 8 were females with M:F ratio of 4:1. The mean age of the recipients was 39 ± 11.6 years old. The recipients’ post-transplant duration ranged from 2 to 80 months (Mean 17.6 ± 18.6 months). Fifteen (37.5%) of the transplant recipients received acyclovir prophylaxis for six months, one recipient (2.5%) received ganciclovir prophylaxis for three weeks while 24 recipients (60%) received no prophylactic therapy. There was no significant difference in the prevalence of seropositive CMV-IgM between transplant recipients who used CMV prophylaxis and those who did not (Fisher exact p = 0.45). <strong>Conclusion:</strong> Prophylaxis with acyclovir for six months showed no significant benefit on post-transplant CMV infection prevention in renal transplant recipients.
文摘This paper aimed at developing a simple and fast approach using chemometrics processing for direct assay of acyclovir in tablets by NIR （near infrared） spectroscopy in diffuse reflectance mode. In making trials with 5 different tablet matrices, the experimental results showed that regardless the matrix variation, it was always possible to construct a quantitative model with suitable linear range, accuracy and precision for direct assay of acyclovir in tablet from NIR spectra. Therefore, the approach used in this study was suitable for on-site fast assay of APIs in tablets during manufacturing process or in post-marketing surveillance of drug quality.
基金The researchers affiliated with the Faculty of Pharmacy,Nootan Pharmacy College,Sankalchand Patel University,Visnagar 384315,Gujarat,India,express their satisfaction,attributing it to the essential resources available that facilitate their research endeavors.
文摘Graphene oxide(GO)and mesoporous silica nanoparticle(MSN)have been documented as advanced nanocarriers for drug delivery due to their unique and versatile properties.The design of GO-MSN nanocomposite offers a large surface area,adjustable pore size,biocompatibility,and low cytotoxicity.The application of acyclovir(ACV)(BCS:III)is suffering from poor permeability,low bioavailability,etc.Hence,the use of GO-MSN nanocomposite for the delivery of ACV may overcome the limitations of ACV.Therefore,the present work aims to design the lipid-coated ACV-loaded GO-MSN(LC-ACV-GO-MSN)nanocomposites.In brief,the design of experiments(DoE,32 response surface methodology)approach was preferred for the development of GO-MSN nanocomposite.The loading of ACV in nanocomposite was done passive loading whereas the coating of lipids was done using a modified thin film hydration technique.At last,different spectral characterizations were performed.The output demonstrated that the entrapment efficiency of ACV-MSN and ACV-GO-MSN was 51.13%and 71.86%,respectively.Afterward,the designed LC-ACV-GO-MSN and ACV-GO-MSN nanocomposite shows 93.40%and 80.74%in vitro drug release,respectively.In conclusion,the design of LC-ACV-GO-MSN nanocomposite using optimized GO-MSN followed lipid coating offers the modified release.Therefore,in the future,LC-ACV-GO-MSN nanocomposite can be used for the delivery of ACV and other drug molecules with a high payload and enhanced release profile.We hope the current proof of concept may provide advantages over existing methods and emphasize the significance of protocells in cargo delivery systems.
