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2012年中国药学大会暨第十二届中国药师周

作者：宋双双沈阳药科大学

本研究的目的是制备一种用于装载难溶性药物的、流动性和稳定性极好的前体囊泡制剂并且评价其作为口服给药系统的生物利用度。将司盘60、胆固醇、山梨醇、长春西汀通过薄膜分散法制备成前体囊泡粉末。将适量的前体囊泡粉末与水混合后,... 详细信息

本研究的目的是制备一种用于装载难溶性药物的、流动性和稳定性极好的前体囊泡制剂并且评价其作为口服给药系统的生物利用度。将司盘60、胆固醇、山梨醇、长春西汀通过薄膜分散法制备成前体囊泡粉末。将适量的前体囊泡粉末与水混合后,囊泡会自发形成。本论文对前体囊泡粉末和由其形成的自主装囊泡混悬液的包封率、粒径、形态学特征、体外溶出和释放、物理稳定性和体内生物利用度进行了评价。前体囊泡粉末具有良好的流动性。投射电子显微镜下观察到由前体囊泡自主装形成的囊泡混悬液呈现圆球状。X射线显示药物以无定形或分子状态存在于前体囊泡粉末中。从体外溶出和释放研究中可看出前体囊泡粉末确实提高了长春西汀的溶出速率和溶出量。而且,自组装的囊泡混悬液显示出缓慢释放药物的特性。与长春西汀混悬液相比,由前体囊泡粉末自主装形成的囊泡混悬液确实提高了长春西汀在新西兰兔中的生物利用度。本研究表明前体囊泡粉末大大提高了制剂的物理和化学稳定性,具有一定的工业前景。

关键词： proniosomes poorly water-soluble drugs vinpocetine reconstituted/proniosome-derived niosomes oral bioavailability

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Enhancement in antinociceptive and anti-inflammatory effects of tramadol by transdermal proniosome gel

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Asian Journal of Pharmaceutical Sciences 2020年第6期15卷 786-796页

作者： Jigar Shah Anroop B.Nair Hiral Shah Shery Jacob Tamer M.Shehata Mohamed Aly Morsy Institute of Pharmacy Nirma UniversityAhmedabad 382481India College of Clinical Pharmacy King Faisal UniversityAl-Ahsa 31982Saudi Arabia Arihant School of Pharmacy&BRI Gandhinagar 382421India College of Pharmacy Gulf Medical UniversityAjman 4184United Arab Emirates Faculty of Pharmacy University of ZagazigZagazig 44519Egypt Faculty of Medicine Minia UniversityEl-Minia 61511Egypt

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.

关键词： Tramadol proniosomes Flux Edema Pharmacokinetics Rats

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Nonionic surfactant vesicular systems for effective drug delivery—an overview

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Acta Pharmaceutica Sinica B 2011年第4期1卷 208-219页

作者： Gannu P.Kumar Pogaku Rajeshwarrao Department of Pharmaceutics Talla Padmavathi College of PharmacyWarangal 506002India

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.

关键词： Niosomes Nonionic surfactants Transferosomes Discomes Elastic niosomes proniosomes

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