Nagaich Upendra, Gulati Neha
Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, U.P., India.
School of Pharmaceutical Sciences, IFTM University, Moradabad, U.P., India.
Curr Drug Deliv. 2018;15(5):641-651. doi: 10.2174/1567201814666170918163615.
Betamethasone Valerate (BV) is a potent topical corticosteroid. Preparation of nanostructured lipid carriers (NLC) involves process parameters optimization and formulations were developed. It is available in several conventional formulations like creams and ointments which have well-known problems of frequent dosing and consequently additional side effects. The aim is to ascertain the probability of NLC as an exclusive carrier for betamethasone valerate topical application with regard to release modulation and improved therapeutic effect.
Preparation of BVNLC formulations involves rigorous broad range optimization of process parameters viz. selection of lipids, surfactants, formulation technique, stirring time, stirring speed and homogenization cycles. Accordingly, optimized parameters were selected and formulation table was developed. Characterizations of developed NLC comprise particle shape, size, zeta potential, percent drug entrapment, in vitro drug release studies. The optimized NLC formulation was gelled and evaluated for ex vivo permeation studies and preclinical anti-inflammatory testing.
The permeation studies revealed that enhancement ratio of BVNLC based gel was 2.59 folds higher as compared to plain BV gel. Release models indicated anomalous (non-fickian) diffusion viz. drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. Preclinical studies indicated a significant (P < 0.05) extended anti-inflammatory effect and 16.5% inhibition compared to plain gel.
The outcome of entire characterization advocates that the developed formulation is efficient as once a day dosing in therapy of atopic dermatitis.
戊酸倍他米松（BV）是一种强效局部用皮质类固醇。纳米结构脂质载体（NLC）的制备涉及工艺参数优化并已开发出相关制剂。它有几种传统剂型，如乳膏和软膏，存在众所周知的频繁给药问题以及随之而来的额外副作用。目的是确定NLC作为戊酸倍他米松局部应用的唯一载体在释放调节和改善治疗效果方面的可能性。
BVNLC制剂的制备涉及对工艺参数进行严格广泛的优化，即脂质、表面活性剂的选择、制剂技术、搅拌时间、搅拌速度和均质化循环。据此，选择了优化参数并制定了制剂表。所开发的NLC的表征包括颗粒形状、大小、zeta电位、药物包封率、体外药物释放研究。将优化后的NLC制剂制成凝胶，并进行离体渗透研究和临床前抗炎测试。
渗透研究表明，与普通BV凝胶相比，基于BVNLC的凝胶的增强率高2.59倍。释放模型表明为非菲克（异常）扩散，即药物释放受不止一个过程控制，即两种现象的叠加，扩散控制以及溶胀控制释放。临床前研究表明，与普通凝胶相比，具有显著（P < 0.05）的延长抗炎作用和16.5%的抑制率。
整个表征结果表明，所开发的制剂在特应性皮炎治疗中每日给药一次是有效的。
