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

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 µm, 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.

Materials

Asiatic acid (95 %) was obtained from SEPPIC, France. Beeswax and cetyl alcohol were purchased from Maximax Pro. Co., Ltd., Thailand. Poloxamer-188 (Kolliphor® P 188, HLB value = 29) was purchased from BASF Pharma, USA. Polysorbate 80 (Tween 80, HLB value = 15), dimethyl sulfoxide (DMSO) extra pure, Brain Heart Infusion (BHI) broth and clindamycin were bought from Merck, Darmstadt, Germany. Soybean L-α Lecithin (soybean lecithin with purity > 94 % phosphatidylcholine and < 2 % triglycerides) from Lipoid.

Romchat Chutoprapat, Jatuporn Witarat, Panalee Jongpanyangarm, Lucy Mang Sung Thluai, Pichanon Khankaew, Lai Wah Chan, Development of solid lipid microparticles (SLMs) containing asiatic acid for topical treatment of acne: Characterization, stability, in vitro and in vivo anti-acne assessment, International Journal of Pharmaceutics, Volume 654, 2024, 123980, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2024.123980.