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使用油酸和硬脂酸的工程化度他雄胺脂质纳米颗粒(DST-LNP)系统用于局部给药。

Engineered Dutasteride-Lipid Based Nanoparticle (DST-LNP) System Using Oleic and Stearic Acid for Topical Delivery.

作者信息

Noor Norhayati Mohamed, Umar Sana, Abdul-Aziz Azila, Sheikh Khalid, Somavarapu Satyanarayana

机构信息

Department of Pharmaceutics, UCL School of Pharmacy, University College London, London WC1N 1AX, UK.

Cosmeceutical & Fragrance Laboratory, Institute of Bioproduct Development (N22), Universiti Teknologi Malaysia, Johor Bahru 81310, Malaysia.

出版信息

Bioengineering (Basel). 2022 Jan 1;9(1):11. doi: 10.3390/bioengineering9010011.

DOI:10.3390/bioengineering9010011
PMID:35049720
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8773293/
Abstract

Male pattern baldness (MPB) is a common condition that has a negative impact on the psycho-social health of many men. This study aims to engineer an alcohol-free formulation to cater for individuals who may have had allergic reactions to alcohol-based preparations. A lipid-based nanoparticle system composed of stearic and oleic acid (solid and liquid lipid) was used to deliver dutasteride (DST) for topical application. Two compositions, with oleic acid (Formulation A) and without (Formulation B), were compared to analyse the role of oleic acid as a potential active ingredient in addition to DST. DST-loaded LNP were prepared using the emulsification-ultrasonication method. All of the prepared formulations were spherical in shape in the nanometric size range (150-300 nm), with entrapment efficiencies of >75%. X-ray diffractograms revealed that DST exists in an amorphous form within the NLP matrices. The drug release behaviour from both LNP preparations displayed slow release of DST. Permeation studies through pig ear skin demonstrated that DST-LNP with oleic acid produced significantly lower permeation into the dermis compared to the formulation without oleic acid. These results suggest that the proposed formulation presents several characteristics which are novel, indicating its suitability for the dermal delivery of anti-androgenic molecules.

摘要

男性型秃发(MPB)是一种常见病症,对许多男性的心理社会健康有负面影响。本研究旨在设计一种无酒精配方,以满足可能对酒精基制剂有过敏反应的个体需求。一种由硬脂酸和油酸(固体和液体脂质)组成的脂质基纳米颗粒系统被用于递送度他雄胺(DST)以供局部应用。比较了两种配方,一种含有油酸(配方A),另一种不含油酸(配方B),以分析除DST外油酸作为潜在活性成分的作用。采用乳化超声法制备了载有DST的脂质纳米颗粒(LNP)。所有制备的配方均为纳米尺寸范围内(150 - 300 nm)的球形,包封率>75%。X射线衍射图显示DST以无定形形式存在于NLP基质中。两种LNP制剂的药物释放行为均显示DST的缓释。通过猪耳皮肤的渗透研究表明,与不含油酸的配方相比,含油酸的DST-LNP向真皮的渗透显著降低。这些结果表明,所提出的配方具有几个新颖的特性,表明其适用于抗雄激素分子的皮肤递送。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/5ecdf30efb96/bioengineering-09-00011-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/33c9aa89f1c1/bioengineering-09-00011-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/28aef384045b/bioengineering-09-00011-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/03c4efe82139/bioengineering-09-00011-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/dca52c3399db/bioengineering-09-00011-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/5ecdf30efb96/bioengineering-09-00011-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/33c9aa89f1c1/bioengineering-09-00011-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/28aef384045b/bioengineering-09-00011-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/03c4efe82139/bioengineering-09-00011-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/dca52c3399db/bioengineering-09-00011-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b403/8773293/5ecdf30efb96/bioengineering-09-00011-g005.jpg

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