Development of solid lipid microparticles (SLMs) containing asiatic acid for topical treatment of acne: Characterization, stability, in vitro and in vivo anti-acne assessment

被引:1
作者
Chutoprapat, Romchat [1 ]
Witarat, Jatuporn [1 ]
Jongpanyangarm, Panalee [1 ]
Thluai, Lucy Mang Sung [1 ]
Khankaew, Pichanon [1 ]
Chan, Lai Wah [2 ]
机构
[1] Chulalongkorn Univ, Dept Pharmaceut & Ind Pharm, Cosmet Sci Program, Fac Pharmaceut Sci, Bangkok 10330, Thailand
[2] Natl Univ Singapore, Dept Pharm, Singapore, Singapore
关键词
Asiatic acid; Solid lipid microparticles; Tween; 80; Soybean lecithin; Poloxamer-188; Anti -acne activity; DRUG-DELIVERY SYSTEMS; ESSENTIAL OIL; CHAIN-LENGTH; SKIN; MICROSPHERES; NANOPARTICLES; CARRIERS; PENETRATION; FORMULATION; RELEASE;
D O I
10.1016/j.ijpharm.2024.123980
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Solid lipid microparticles (SLMs) represent a promising approach for drug delivery in anti -acne applications. In this study, asiatic acid -loaded SLMs (AASLMs) were prepared by melt emulsification method in conjunction with freeze-drying. Comprehensive evaluations comprised particle size, %entrapment efficiency (%EE), %labeled amount (%LA), surface morphology, stability, %release, %skin permeation, and anti -acne activity. The AASLMs exhibited an average particle size ranging from 7.46 to 38.86 mu m, with %EE and %LA falling within the range of 31.56 to 100.00 and 90.43 to 95.38, respectively. The AASLMs demonstrated a spherical shape under scanning electron microscopy, and maintained stability over a 3 -month period. Notably, formulations with 10 % and 15 % cetyl alcohol stabilized with poloxamer-188 (specifically F6 and F12) displayed a minimum inhibitory concentration (MIC) value of 75 mg/ml against Cutibacterium acnes . Furthermore, F12 exhibited a higher %release and %skin permeation compared to F6 over 24 h. In a single-blind clinical trial involving fifteen participants with mild -to -moderate acne, F12 showcased its potential not only in reducing porphyrin intensity and enhancing skin barriers but also in significantly improving skin hydration and brightness. However, further investigations with larger subject cohorts encompassing diverse age groups and genders are necessary to thoroughly establish the performance of the developed AASLMs.
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页数:18
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共 110 条
[1]  
Abu-Qatouseh Luay, 2019, Biomedical & Pharmacology Journal, V12, P211, DOI 10.13005/bpj/1629
[2]   Lyophilized Drug-Loaded Solid Lipid Nanoparticles Formulated with Beeswax and Theobroma Oil [J].
Amekyeh, Hilda ;
Billa, Nashiru .
MOLECULES, 2021, 26 (04)
[3]   Animal models of skin disease for drug discovery [J].
Avci, Pinar ;
Sadasivam, Magesh ;
Gupta, Asheesh ;
De Melo, Wanessa C. M. A. ;
Huang, Ying-Ying ;
Yin, Rui ;
Chandran, Rakkiyappan ;
Kumar, Raj ;
Otufowora, Ayodeji ;
Nyame, Theodore ;
Hamblin, Michael R. .
EXPERT OPINION ON DRUG DISCOVERY, 2013, 8 (03) :331-355
[4]   Liquid Lipids Act as Polymorphic Modifiers of Tristearin-Based Formulations Produced by Melting Technologies [J].
Bertoni, Serena ;
Passerini, Nadia ;
Albertini, Beatrice .
PHARMACEUTICS, 2021, 13 (07)
[5]   Penetration of drugs through skin, a complex rate-controlling membrane [J].
Bolzinger, Marie-Alexandrine ;
Briancon, Stephanie ;
Pelletier, Jocelyne ;
Chevalier, Yves .
CURRENT OPINION IN COLLOID & INTERFACE SCIENCE, 2012, 17 (03) :156-165
[6]  
Bone K., 2012, Principles and practice of phytotherapy: modern herbal medicine, V2, DOI DOI 10.1016/B978-0-443-06992-5.00001-3
[7]   The anti-inflammatory effects of asiatic acid in lipopolysaccharide-stimulated human corneal epithelial cells [J].
Chen, Hao ;
Hua, Xiao-Min ;
Ze, Bai-Chen ;
Wang, Bin ;
Wei, Li .
INTERNATIONAL JOURNAL OF OPHTHALMOLOGY, 2017, 10 (02) :179-185
[8]   Formulation and evaluation of a topical liposomal gel containing a combination of zedoary turmeric oil and tretinoin for psoriasis activity [J].
Chen, Ji ;
Ma, Yanqiao ;
Tao, Yueying ;
Zhao, Xiaoqian ;
Xiong, Yongai ;
Chen, Zehui ;
Tian, Yingbiao .
JOURNAL OF LIPOSOME RESEARCH, 2021, 31 (02) :130-144
[9]   Preparation and evaluation of PEGylated asiatic acid nanostructured lipid carriers on anti-fibrosis effects [J].
Chen, Xiaoxiao ;
Zhang, Yawen ;
Zhao, Pengfei ;
Chen, Yan ;
Zhou, Yunli ;
Wang, Shenghao ;
Yin, Lina .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2020, 46 (01) :57-69
[10]   A Mini-Review on Solid Lipid Nanoparticles and Nanostructured Lipid Carriers: Topical Delivery of Phytochemicals for the Treatment of Acne Vulgaris [J].
Chutoprapat, Romchat ;
Kopongpanich, Peerawas ;
Chan, Lai Wah .
MOLECULES, 2022, 27 (11)