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
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.
