Smeu Andreea, Minda Daliana, Boru Casiana, Vlaia Lavinia, Vlaia Vicențiu, Dehelean Cristina Adriana, Liga Sergio, Puenea George, Muntean Daniela Lucia
Research Centre for Pharmaco-Toxicological Evaluation, Faculty of Pharmacy, "Victor Babes" University of Medicine and Pharmacy, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
Discipline of Toxicology, Drug Industry, Management and Legislation, Faculty of Pharmacy, "Victor Babeş" University of Medicine and Pharmacy Timisoara, 2nd Eftimie Murgu Square, 300041 Timisoara, Romania.
Life (Basel). 2025 Jun 13;15(6):954. doi: 10.3390/life15060954.
Skin disorders constitute a persistent health problem, covering both acute and chronic conditions that manifest in patients of all ages. Betulinic acid (BA) is a triterpene previously studied as an efficient treatment of skin ailments due to its innate pharmacological properties. Nonetheless, due to its lipophilic nature and low bioavailability, topical delivery systems are necessary for its proper administration. Oleogels are efficient carriers for the incorporation of hydrophobic biomolecules; however, their use for the delivery of BA remains scarce. Therefore, this study was designed to develop, characterize, and evaluate a BA-containing oleogel (BA-O) regarding its cutaneous safety profile as a potential pharmaceutical formulation targeting dermatologic issues. The findings illustrated the efficient formulation of BA as oleogel, the product presenting the specific conditions of topical semi-solid formulations in terms of physico-chemical characteristics and high biocompatibility in vitro and in ovo, as BA-O lacked a cytotoxic effect in HaCaT and JB6 Cl 41-5a skin cells (cell viability percentages being > 70%) and was categorized as non-irritant in EpiDerm™ tissues (viability > 80%) and on the chorioallantoic membrane (Irritation Score = 0.186). These results present the preclinical biosafety profile of BA-O with prospective potential for cutaneous applications that should be investigated in future studies.
皮肤疾病是一个持续存在的健康问题，涵盖了所有年龄段患者中出现的急性和慢性病症。桦木酸（BA）是一种三萜类化合物，由于其固有的药理特性，此前被研究作为治疗皮肤疾病的有效药物。然而，由于其亲脂性和低生物利用度，需要局部给药系统来进行适当的给药。油凝胶是用于掺入疏水性生物分子的有效载体；然而，将其用于BA的递送仍然很少见。因此，本研究旨在开发、表征和评估一种含BA的油凝胶（BA-O），作为一种针对皮肤问题的潜在药物制剂，评估其皮肤安全性。研究结果表明，BA作为油凝胶的有效制剂，该产品在物理化学特性方面呈现出局部半固体制剂的特定条件，并且在体外和卵内具有高生物相容性，因为BA-O在HaCaT和JB6 Cl 41-5a皮肤细胞中没有细胞毒性作用（细胞活力百分比>70%），并且在EpiDerm™组织中被归类为无刺激性（活力>80%），在绒毛尿囊膜上也是如此（刺激评分=0.186）。这些结果展示了BA-O的临床前生物安全性，具有在皮肤应用方面的潜在前景，应在未来的研究中进行进一步研究。
