Khan Sana, Jain Poorva, Jain Sourabh, Jain Richa, Bhargava Saurabh, Jain Aakanchha
Bhagyoday Tirth Pharmacy College, Sagar (M.P.), India.
Centre for Scientific Research and Development, People's University, Bhopal (M.P.), India.
Pharm Nanotechnol. 2018;6(1):38-47. doi: 10.2174/2211738506666180209100222.
Topical delivery is an attractive route for local and systemic treatment. The novel topical application has many advantages like averting the GI-irritation, preventing the metabolism of drugs in the liver and increasing the bioavailability of the drug over the conventional dosage forms.
The aim of present work was to prepare and characterized erythromycin encapsulated cubosomes using different concentrations of glyceryl monooleate and poloxamer 407 by the emulsification method.
The prepared dispersion of cubosomes was characterized for surface morphology, particle size, entrapment efficiency and in vitro release. Further, optimized formulation was converted to cubosomal gel by incorporating carbopol 934 at different concentrations. The prepared gel was characterized for homogeneity, pH, viscosity, spreadibility, drug content and in vitro drug release study.
The result of optimized cubosomes showed average particle size of 264.5±2.84nm and entrapment efficiency about 95.29±1.32 % and the pH of optimized cubosomal was found to be 6.5, viscosity 2475-8901(cp), drug content 95.29% and the spreadability was found to be 11.74 gm.cm/sec. The in vitro drug release kinetics of optimized formulation was found to follow Korsmeyer peppas model having highest R2 value 0.835 and in vitro drug release of optimized erythromycin loaded cubosomal gel and plain drug gel in 24 hr was found to be 89.91±0.73 and 88.64±2.16, while in 36 hr plain drug gel and cubosomal gel showed drug release about 87.64±0.97 and 91.55±1.09, and sustained release was obtained after 24 hr in case of cubosomal gel.
Thus, as a whole it can be concluded that erythromycin loaded cubosomes are effective in topically delivering drug in sustained and non-invasive manner for treatment and prevention of acne.
局部给药是局部和全身治疗的一种有吸引力的途径。新型局部应用具有许多优点，如避免胃肠道刺激、防止药物在肝脏中代谢以及比传统剂型提高药物的生物利用度。
本研究的目的是通过乳化法使用不同浓度的单油酸甘油酯和泊洛沙姆407制备并表征包封红霉素的立方液晶纳米粒。
对制备的立方液晶纳米粒分散体进行表面形态、粒径、包封率和体外释放的表征。此外，通过加入不同浓度的卡波姆934将优化后的制剂转化为立方液晶纳米粒凝胶。对制备的凝胶进行均匀性、pH值、粘度、铺展性、药物含量和体外药物释放研究的表征。
优化后的立方液晶纳米粒平均粒径为264.5±2.84nm，包封率约为95.29±1.32%，优化后的立方液晶纳米粒pH值为6.5，粘度为2475 - 8901（厘泊），药物含量为95.29%，铺展性为11.74克·厘米/秒。优化后的制剂体外药物释放动力学符合Korsmeyer - peppas模型，R²值最高为0.835，优化后的载红霉素立方液晶纳米粒凝胶和普通药物凝胶在24小时内的体外药物释放分别为89.91±0.73和88.64±2.16，而在36小时时普通药物凝胶和立方液晶纳米粒凝胶的药物释放分别约为87.64±0.97和91.55±1.09，立方液晶纳米粒凝胶在24小时后实现了持续释放。
因此，总体而言，可以得出结论，载红霉素的立方液晶纳米粒能够以持续且非侵入性的方式有效局部递送药物，用于痤疮的治疗和预防。
