Oral therapy of tramadol,an opiate analgesic,undergoes extensive hepatic metabolism and requires frequent administration.Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce ...Oral therapy of tramadol,an opiate analgesic,undergoes extensive hepatic metabolism and requires frequent administration.Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol.The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo.The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined.Best proniosome gel(F4)was selected and evaluated for drug release,stability and transdermal efficacy by ex vivo and in vivo experiments.The vesicles demonstrated optimal properties including spherical shape,nanosize with good entrapment efficiency,adequate zeta potential,higher stability and greater transdermal flux.The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter.Release profile of F4 was distinct(P<0.001)from control and displayed steady and prolonged tramadol release by Fickian diffusion.Transdermal therapy of F4 showed prominent reduction of induced twitches(P<0.005)in mice and edema(P<0.05)in rats,as compared to oral tramadol.The improvement in clinical efficacy of tramadol in transdermal therapy is correlated with the pharmacokinetic data observed.In conclusion,the observed improvement in antinociceptive and anti-inflammatory effects from proniosome carriers signifies its potential to be a suitable alternative to oral therapy of tramadol with greater efficacy.展开更多
Vesicular systems are a novel means of drug delivery that can enhance bioavailability of encapsulated drug and provide therapeutic activity in a controlled manner for a prolonged period of time.Liposomes were the firs...Vesicular systems are a novel means of drug delivery that can enhance bioavailability of encapsulated drug and provide therapeutic activity in a controlled manner for a prolonged period of time.Liposomes were the first such system but they suffer from a number of drawbacks including high cost and lack of stability at various pHs.Niosomes are a nonionic surfactant vesicular system,which can be easily and reliably made in the laboratory.Many factors affect noisome formation such as the method of manufacture,nature of surfactant and encapsulated drug,temperature at which the lipids are hydrated and the critical packing parameter.This review describes all aspects of niosomes including their different compositions,the various methods of preparation,the effect of changing manufacturing parameters,methods of characterization,factors that affect their stability,their use by various routes of administration,their therapeutic applications and the most important patents.The review also provides detailed information of the various types of niosomes that provide effective drug delivery.展开更多
Proniosomes are drug-encapsulated,nanoscale vesicular structures that generate multilamellar niosomal dispersions upon hydration.This study aimed to develop enalapril maleate nanoproniosomal gels and assess their effe...Proniosomes are drug-encapsulated,nanoscale vesicular structures that generate multilamellar niosomal dispersions upon hydration.This study aimed to develop enalapril maleate nanoproniosomal gels and assess their effectiveness in experimental hypertensive rat models.The gels were synthesized based on the coacervation phase separation method,using lecithin,cholesterol,and various nonionic surfactants as formulation components,along with the drug.The developed gels were then subjected to various analyses,such as pH,viscosity,rate of spontaneity,entrapment efficiency,vesicle size,ex vivo permeation,skin irritation,scanning electron microscopy,stability,in vivo bio-availability,in vivo antihypertensive activity,and in vitro-in vivo correlation studies.Results revealed that all synthesized gel formulations maintained good physical characteristics,within permissible limits.The results of the ex vivo skin permeation analysis revealed non-Fickian release kinetics and zero-order penetration behaviors of the drug formulations with diffusion,achieving a cumulative permeation rate of 58.75%-89.72%through albino rat skin over 24 h.Moreover,skin irritation tests revealed that the topical application of the drug formulations did not cause any signs of irritation,indicating their safety.Furthermore,in vivo bio-availability studies revealed that one particular formulation,EMNP7,demonstrated an approximately 188.99-fold greater bio-availability compared to the Vasotec tablet.Additionally,in vivo antihypertensive analysis revealed that this formulation effectively restored elevated rat blood pressures to the normal range.Furthermore,the in vitro-in vivo correlation analysis suggested that the ex vivo(in vitro)data could accurately replicate in vivo physiological conditions.Overall,our findings indicate that enalapril maleate encapsulated within nanoproniosomal gels can effectively function as controlled drug delivery systems,releasing the drug once per day for effective hypertension management.展开更多
Febuxostat(FXT)is useful in treating hyperuricemia and chronic gout.However,it has limited bioavailability orally due to its low solubility and short half-life.This results in the need for more frequent and larger dos...Febuxostat(FXT)is useful in treating hyperuricemia and chronic gout.However,it has limited bioavailability orally due to its low solubility and short half-life.This results in the need for more frequent and larger doses,increasing the likelihood of adverse effects.Against this background,the current study was established to prepare and optimize an FXT-loaded proniosomal gel using the coacervation-phase separation method.A Quality-by-Design(QbD)methodology was used to ensure the quality of the finished product by assessing how critical process parameters and critical material attributes(CMAs)affected the proniosomal gel’s critical quality attributes.Box-Behnken design was employed to explore the effect of CMAs such as the amount of cholesterol,Span 40,and Span 60 on particle size and entrapment efficiency.The optimized proniosomes had a particle size and percentage entrapment efficiency of 193.7±2.26 nm and 85.3%±0.89%,respectively.Scanning electron microscopy was used to examine the surface morphology of the optimized formulation.The developed formulation was also subjected to in vitro drug release and ex vivo permeation studies,which established the efficiency of the prepared proniosomal gel.Stability studies also established the fact that the prepared formulation is stable to variations in temperature for up to 6 months.展开更多
文摘Oral therapy of tramadol,an opiate analgesic,undergoes extensive hepatic metabolism and requires frequent administration.Transdermal therapy by virtue can overcome these issues and can improve the efficacy and reduce abuse liability of tramadol.The aim of this research was to investigate the possibility of transdermal delivery of tramadol by formulating proniosome gel and evaluate its therapeutic potential in vivo.The effect of formulation composition as well as amount of drug on physicochemical characteristics of prepared proniosomes were examined.Best proniosome gel(F4)was selected and evaluated for drug release,stability and transdermal efficacy by ex vivo and in vivo experiments.The vesicles demonstrated optimal properties including spherical shape,nanosize with good entrapment efficiency,adequate zeta potential,higher stability and greater transdermal flux.The amorphization and dispersion of tramadol in the aqueous core of proniosome vesicles was confirmed by differential scanning calorimeter.Release profile of F4 was distinct(P<0.001)from control and displayed steady and prolonged tramadol release by Fickian diffusion.Transdermal therapy of F4 showed prominent reduction of induced twitches(P<0.005)in mice and edema(P<0.05)in rats,as compared to oral tramadol.The improvement in clinical efficacy of tramadol in transdermal therapy is correlated with the pharmacokinetic data observed.In conclusion,the observed improvement in antinociceptive and anti-inflammatory effects from proniosome carriers signifies its potential to be a suitable alternative to oral therapy of tramadol with greater efficacy.
文摘Vesicular systems are a novel means of drug delivery that can enhance bioavailability of encapsulated drug and provide therapeutic activity in a controlled manner for a prolonged period of time.Liposomes were the first such system but they suffer from a number of drawbacks including high cost and lack of stability at various pHs.Niosomes are a nonionic surfactant vesicular system,which can be easily and reliably made in the laboratory.Many factors affect noisome formation such as the method of manufacture,nature of surfactant and encapsulated drug,temperature at which the lipids are hydrated and the critical packing parameter.This review describes all aspects of niosomes including their different compositions,the various methods of preparation,the effect of changing manufacturing parameters,methods of characterization,factors that affect their stability,their use by various routes of administration,their therapeutic applications and the most important patents.The review also provides detailed information of the various types of niosomes that provide effective drug delivery.
文摘Proniosomes are drug-encapsulated,nanoscale vesicular structures that generate multilamellar niosomal dispersions upon hydration.This study aimed to develop enalapril maleate nanoproniosomal gels and assess their effectiveness in experimental hypertensive rat models.The gels were synthesized based on the coacervation phase separation method,using lecithin,cholesterol,and various nonionic surfactants as formulation components,along with the drug.The developed gels were then subjected to various analyses,such as pH,viscosity,rate of spontaneity,entrapment efficiency,vesicle size,ex vivo permeation,skin irritation,scanning electron microscopy,stability,in vivo bio-availability,in vivo antihypertensive activity,and in vitro-in vivo correlation studies.Results revealed that all synthesized gel formulations maintained good physical characteristics,within permissible limits.The results of the ex vivo skin permeation analysis revealed non-Fickian release kinetics and zero-order penetration behaviors of the drug formulations with diffusion,achieving a cumulative permeation rate of 58.75%-89.72%through albino rat skin over 24 h.Moreover,skin irritation tests revealed that the topical application of the drug formulations did not cause any signs of irritation,indicating their safety.Furthermore,in vivo bio-availability studies revealed that one particular formulation,EMNP7,demonstrated an approximately 188.99-fold greater bio-availability compared to the Vasotec tablet.Additionally,in vivo antihypertensive analysis revealed that this formulation effectively restored elevated rat blood pressures to the normal range.Furthermore,the in vitro-in vivo correlation analysis suggested that the ex vivo(in vitro)data could accurately replicate in vivo physiological conditions.Overall,our findings indicate that enalapril maleate encapsulated within nanoproniosomal gels can effectively function as controlled drug delivery systems,releasing the drug once per day for effective hypertension management.
文摘Febuxostat(FXT)is useful in treating hyperuricemia and chronic gout.However,it has limited bioavailability orally due to its low solubility and short half-life.This results in the need for more frequent and larger doses,increasing the likelihood of adverse effects.Against this background,the current study was established to prepare and optimize an FXT-loaded proniosomal gel using the coacervation-phase separation method.A Quality-by-Design(QbD)methodology was used to ensure the quality of the finished product by assessing how critical process parameters and critical material attributes(CMAs)affected the proniosomal gel’s critical quality attributes.Box-Behnken design was employed to explore the effect of CMAs such as the amount of cholesterol,Span 40,and Span 60 on particle size and entrapment efficiency.The optimized proniosomes had a particle size and percentage entrapment efficiency of 193.7±2.26 nm and 85.3%±0.89%,respectively.Scanning electron microscopy was used to examine the surface morphology of the optimized formulation.The developed formulation was also subjected to in vitro drug release and ex vivo permeation studies,which established the efficiency of the prepared proniosomal gel.Stability studies also established the fact that the prepared formulation is stable to variations in temperature for up to 6 months.
