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1.
Int J Pharm ; 654: 123980, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38460769

RESUMO

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.


Assuntos
Acne Vulgar , Sistemas de Liberação de Medicamentos , Triterpenos Pentacíclicos , Feminino , Humanos , Masculino , Acne Vulgar/tratamento farmacológico , Portadores de Fármacos , Sistemas de Liberação de Medicamentos/métodos , Lipídeos , Tamanho da Partícula , Método Simples-Cego
2.
Int J Pharm ; 651: 123738, 2024 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-38158144

RESUMO

Non-invasive treatment options for hypertrophic scars (HTS) are limited, and treating HTS remains challenging due to their unappealing appearance and associated social stigma. In this work, a novel transfersomal system named Asiatic acid-entrapped transfersomes (AATs) was prepared. AATs were evaluated for their skin permeability, anti-inflammatory activity, and other characteristic parameters to determine the most promising formulation. Asiatic acid-entrapped transfersomal gel (AATG), which was obtained by incorporating the lead AATs in a gel base, underwent testing in an 8-week, double-blind, placebo-controlled, split-skin clinical study. The net skin elasticity (R5), melanin index (MI), and skin surface hydration were analyzed employing Cutometer®, Mexameter®, and Corneometer®, respectively, in order to evaluate the effectiveness of the developed AATG. AATs exhibited vesicular sizes and zeta potential values within the range of (27.15 ± 0.95 to 63.54 ± 2.51 nm) and (-0.010 to -0.129 mV), respectively. TW80AAT gave the highest %EE (90.84 ± 2.99%), deformability index (101.70 ± 11.59 mgs-1), permeation flux at 8 h (0.146 ± 0.005 mg/cm2/h), and anti-inflammatory activity (71.65 ± 1.83%). The clinical study results of AATG indicated no adverse skin reactions. Furthermore, product efficacy tests demonstrated a significant reduction in MI and an increase in net skin elasticity at 2, 4, and 8 weeks. These pilot study outcomes support the effectiveness of the AATG.


Assuntos
Cicatriz Hipertrófica , Lipossomos , Triterpenos Pentacíclicos , Humanos , Administração Cutânea , Anti-Inflamatórios , Cicatriz Hipertrófica/patologia , Método Duplo-Cego , Projetos Piloto , Pele/patologia
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