Bharadwaj Rituraj, Das Pranab Jyoti, Pal Paulami, Mazumder Bhaskar
a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dibrugarh University , Dibrugarh , Assam , India.
Drug Dev Ind Pharm. 2016 Sep;42(9):1482-94. doi: 10.3109/03639045.2016.1151028. Epub 2016 Mar 4.
Skin cancer represents the most growing types of cancer in human and ultraviolet radiation can be cited as one of the prime factor for its occurrence. Current therapy of skin cancer suffers from numerous side effects; for effective therapy, topical application of formulation of paclitaxel (PTX) can be considered as a novel approach.
The present study is an attempt to prepare formulation of solid lipid nanoparticles (SLN) of PTX for the effective treatment of various form of skin carcinoma.
The SLN were prepared by high-speed homogenization and ultrasonication method. The prepared SLN were characterized. The optimized PTX SLN were loaded in carbopol gel. The prepared gels were evaluated for its gelling properties and finally studied for in vivo anti-cancer efficacy and histopathological study.
The particle size distribution was found to be in the range of 78.82-587.8 nm. The product yield (%) was found between 60% and 66% and showed a highest entrapment efficiency of 68.3%. The in vitro release of the drug from SLN dispersion was found to be biphasic with the initial burst effect, followed by slow release. SLN-loaded gel were subjected to permeability study and the results show steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio were significantly increased in SLN-loaded gel formulation as compared with PTX-loaded gel. The histopathological study clearly reveals the efficacy of the SLN-F3 3G in the treatment of skin cancer.
The experimental formulations show controlled release of PTX and thus expected to show reduce dose-related side effects.
皮肤癌是人类中增长最快的癌症类型之一，紫外线辐射可被视为其发生的主要因素之一。目前的皮肤癌治疗存在许多副作用；为了实现有效治疗，紫杉醇（PTX）制剂的局部应用可被视为一种新方法。
本研究旨在制备PTX固体脂质纳米粒（SLN）制剂，以有效治疗各种形式的皮肤癌。
通过高速均质和超声法制备SLN。对制备的SLN进行表征。将优化后的PTX SLN负载于卡波姆凝胶中。对制备的凝胶进行凝胶特性评估，最后研究其体内抗癌疗效和组织病理学。
发现粒径分布在78.82 - 587.8nm范围内。产品收率（%）在60%至66%之间，包封率最高达68.3%。药物从SLN分散体中的体外释放呈双相，有初始突释效应，随后缓慢释放。对负载SLN的凝胶进行渗透性研究，结果表明，与负载PTX的凝胶相比，负载SLN的凝胶制剂的稳态通量（Jss）、渗透系数（Kp）和增强比均显著增加。组织病理学研究清楚地揭示了SLN-F3 3G在治疗皮肤癌方面的疗效。
实验制剂显示PTX的控释，因此有望减少剂量相关的副作用。
