Verma Shivani, Utreja Puneet
Department of Pharmaceutics, Rayat-Bahra College of Pharmacy, Hoshiarpur, Punjab 146001, India
Research Scholar, I.K. Gujral Punjab Technical University, Jalandhar-Punjab 144601, India
Pharm Nanotechnol. 2018;6(3):171-179. doi: 10.2174/2211738506666180813122102.
Transdermal drug delivery is an attractive approach for both local and systemic therapeutics of various diseases. Transdermal drug delivery systems show various advantages like reduction of local irritation, prevention of first-pass hepatic metabolism, and bioavailability enhancement of bioactive molecules over conventional drug delivery systems.
The main objective of the present research work was to develop and characterize (in-vitro and ex-vivo) econazole nitrate loaded transethosomes and their comparison with marketed cream of econazole nitrate [Ecoderm, Brown and Burk Pharmaceutical (Pvt.) Ltd., Bengaluru, India] for effective transdermal delivery.
Transethosomes loaded with econazole nitrate were developed by homogenization method and evaluated for entrapment (%), vesicular size, zeta potential, polydispersity index (PDI), and invitro drug release. Furthermore, optimized econazole nitrate loaded transethosomes were added to Carbopol 934 gel and this gel was evaluated for viscosity, pH, drug content, ex-vivo skin permeation and retention studies followed by in-vitro antifungal activity against C. albicans fungus.
The optimized transethosomes loaded with econazole nitrate showed vesicle size of 159.3 ± 4.3 nm, entrapment efficiency about 78.3 ± 2.8%, acceptable colloidal properties like (zeta potential = -27.13 ± 0.33 mV, PDI = 0.244 ± 0.045), approximately 57.56 ± 2.33% drug release up to 24 h. Results of DSC analysis confirmed the encapsulation of econazole nitrate inside transethosomes. Optimized transethosomes showed drug release following zero order through diffusion mechanism. Transethosomal gel showed high drug content (92.35 ± 0.63%) and acceptable values of pH (5.68 ± 0.86) or viscosity (10390 ± 111 cPs). Transethosomal gel showed less ex-vivo skin penetration (17.53 ± 1.20%), high ex-vivo skin retention (38.75 ± 2.88%), and high in-vitro antifungal activity compared to the marketed cream of econazole nitrate.
Therefore, it can be concluded that econazole nitrate loaded transethosomes are effective to deliver econazole nitrate transdermally in a controlled fashion for effective elimination of cutaneous candidiasis.
经皮给药是治疗各种疾病的局部和全身疗法的一种有吸引力的方法。与传统给药系统相比，经皮给药系统具有多种优势，如减少局部刺激、防止首过肝代谢以及提高生物活性分子的生物利用度。
本研究工作的主要目的是开发载有硝酸益康唑的转质体并对其进行（体外和离体）表征，并将其与市售硝酸益康唑乳膏[Ecoderm，Brown and Burk制药（私人）有限公司，印度班加罗尔]进行比较，以实现有效的经皮给药。
采用匀化法制备载有硝酸益康唑的转质体，并对其包封率（%）、囊泡大小、zeta电位、多分散指数（PDI）和体外药物释放进行评估。此外，将优化后的载有硝酸益康唑的转质体加入卡波姆934凝胶中，并对该凝胶的粘度、pH值、药物含量、离体皮肤渗透和滞留进行研究，随后对其对白色念珠菌的体外抗真菌活性进行评估。
优化后的载有硝酸益康唑的转质体囊泡大小为159.3±4.3nm，包封效率约为78.3±2.8%，具有可接受的胶体性质（zeta电位=-27.13±0.33mV，PDI=0.244±0.045），在24小时内药物释放约为57.56±2.33%。差示扫描量热法（DSC）分析结果证实硝酸益康唑被包封在转质体内。优化后的转质体通过扩散机制呈现零级药物释放。转质体凝胶显示出高药物含量（92.35±0.63%）以及可接受的pH值（5.68±0.86）或粘度值（10390±111cPs）。与市售硝酸益康唑乳膏相比，转质体凝胶显示出较低的离体皮肤渗透率（17.53±1.20%）、较高的离体皮肤滞留率（38.75±2.88%）和较高的体外抗真菌活性。
因此，可以得出结论，载有硝酸益康唑的转质体能够有效地以可控方式经皮递送硝酸益康唑，从而有效消除皮肤念珠菌病。
