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糠酸莫米松固体脂质纳米粒用于局部给药的研发与评价

Development and evaluation of solid lipid nanoparticles of mometasone furoate for topical delivery.

作者信息

Madan Jyotsana R, Khude Priyanka A, Dua Kamal

机构信息

Department of Pharmaceutics, Sinhgad Technical Education Society's Smt, Kashibai Navale College of Pharmacy, Pune, Maharashtra, India.

Department of Pharmaceutical Technology, School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur, Malaysia.

出版信息

Int J Pharm Investig. 2014 Apr;4(2):60-4. doi: 10.4103/2230-973X.133047.

DOI:10.4103/2230-973X.133047
PMID:25006550
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4083535/
Abstract

INTRODUCTION

Solid lipid nanoparticles (SLNs) are the new generation of submicron sized lipid emulsions where liquid lipid (oil) has been substituted by solid lipid. Lipids used in the formulation are safe, stable and biodegradable in nature. SLNs offer various advantages for topical drug delivery like ability of deposition into skin with the reduced systemic exposure and reduced local side-effects along with providing sustained release of drug. Mometasone furoate (MF) is a topical glucocorticoid having anti-inflammatory, anti-pruritic, anti-hyper proliferative activity. Owing to these properties it is recommended in chronic inflammation and psoriasis. In market, MF cream and lotion (0.1%) are available, which show slight skin irritation, burning and common side-effects due to steroids.

EXPERIMENTAL

To overcome the shortcomings of conventional formulations, there is a need to develop a novel formulation that can reduce these side-effects and show maximum desired effects. Thus, SLN of MF can be prepared, which would help in increasing skin deposition as well as provide sustained release. In this study, SLNs were prepared by solvent - injection method.

RESULTS

The F8 batch had shown maximum entrapment up to55.59% and sustained drug release for more than 8 h. The skin permeability of SLN loaded gel was found to be 15.21times more than that of marketed cream. SLN loaded gel showed 83.52% of skin deposition which was 2.67 times more than marketed cream and 20 times more than plain drug loaded gel. The scanning electron microscopy and zeta potential study showed formation of good SLN dispersion. The stability study showed successful formation of stable SLNs. Thus, SLNs proved the potential for topical delivery of corticosteroid drug over the conventional formulations.

EXPERIMENTAL

To overcome the shortcomings of conventional formulations, there is a need to develop a novel formulation that can reduce these side-effects and show maximum desired effects. Thus, SLN of MF can be prepared, which would help in increasing skin deposition as well as provide sustained release. In this study, SLNs were prepared by solvent - injection method.

摘要

引言

固体脂质纳米粒(SLNs)是新一代亚微米级脂质乳剂,其中液态脂质(油)已被固体脂质取代。制剂中使用的脂质本质上安全、稳定且可生物降解。SLNs为局部给药提供了多种优势,如能够沉积到皮肤中,减少全身暴露,降低局部副作用,同时实现药物的持续释放。糠酸莫米松(MF)是一种具有抗炎、止痒、抗增殖活性的局部糖皮质激素。由于这些特性,它被推荐用于慢性炎症和银屑病。市场上有MF乳膏和洗剂(0.1%),但由于含有类固醇,会有轻微的皮肤刺激、灼烧感和常见的副作用。

实验

为了克服传统制剂的缺点,需要开发一种新型制剂,以减少这些副作用并展现出最大的预期效果。因此,可以制备MF的SLN,这将有助于增加皮肤沉积并实现持续释放。在本研究中,通过溶剂注射法制备了SLNs。

结果

F8批次显示出最高包封率,可达55.59%,并能持续释药超过8小时。载有SLN的凝胶的皮肤渗透率比市售乳膏高15.21倍。载有SLN的凝胶显示出83.52%的皮肤沉积率,这比市售乳膏高约2.67倍,比普通载药凝胶高20倍。扫描电子显微镜和zeta电位研究表明形成了良好的SLN分散体。稳定性研究表明成功制备出了稳定的SLNs。因此,与传统制剂相比,SLNs证明了其在局部递送皮质类固醇药物方面的潜力。

实验

为了克服传统制剂的缺点需要开发一种新型制剂,以减少这些副作用并展现出最大的预期效果。因此,可以制备MF的SLN,这将有助于增加皮肤沉积并实现持续释放。在本研究中,通过溶剂注射法制备了SLNs。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/b113c121955e/IJPI-4-60-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/99f298a6e751/IJPI-4-60-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/940bd843a640/IJPI-4-60-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/b699470538ad/IJPI-4-60-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/b113c121955e/IJPI-4-60-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/99f298a6e751/IJPI-4-60-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/940bd843a640/IJPI-4-60-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/b699470538ad/IJPI-4-60-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/114c/4083535/b113c121955e/IJPI-4-60-g009.jpg

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