Souza Aleph M S, Ribeiro Renato C A, Pinheiro Gleyse K L O, Pinheiro Francisco I, Oliveira Wógenes N, Souza Luanda B F C, Silva André L, Amaral-Machado Lucas, Alencar Éverton N, Chaves Guilherme M, Egito Eryvaldo S T
Graduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Norte (UFRN), Natal 59012-570, Brazil.
Graduate Program in Health Sciences, Federal University of Rio Grande do Norte (UFRN), Natal 59012-570, Brazil.
Pharmaceutics. 2021 May 24;13(6):784. doi: 10.3390/pharmaceutics13060784.
Onychomycosis induced by spp. has several limitations regarding its treatment. Nail lacquers display the potential to overcome these drawbacks by providing therapeutic compliance and increasing local drug bioavailability. Thus, this work aimed to produce a nail lacquer loaded with Amphotericin B (AmB) and evaluate its performance. The AmB-loaded nail lacquer was produced and preliminarily characterized. An AmB quantification method was developed. Stability, drug release, permeability and anti- activity assays were conducted. The analytical method validation met the acceptance criteria. The drug loading efficiency was 100% (0.02 mg/g of total product), whereas the AmB stability was limited to ≅7 days (≅90% remaining). The nail lacquer displayed a drying time of 187 s, non-volatile content of around 20%, water-resistance of approximately 2% of weight loss and satisfactory in vitro adhesion. Moreover, the in vitro antifungal activity against different spp. strains was confirmed. The AmB release and the ex vivo permeability studies revealed that AmB leaves the lacquer and permeates the nail matrix in 47.76 ± 0.07% over 24 h. In conclusion, AmB-loaded nail lacquer shows itself as a promising extemporaneous dosage form with remarkable anti- activity related to onychomycosis.
由 种引起的甲癣在治疗方面存在若干局限性。指甲油通过提供治疗依从性和提高局部药物生物利用度，显示出克服这些缺点的潜力。因此，本研究旨在制备一种载有两性霉素B（AmB）的指甲油并评估其性能。制备了载有AmB的指甲油并进行了初步表征。开发了一种AmB定量方法。进行了稳定性、药物释放、渗透性和抗活性测定。分析方法验证符合验收标准。载药效率为100%（每克总产品含0.02毫克），而AmB的稳定性限制在约7天（剩余约90%）。该指甲油的干燥时间为187秒，非挥发性含量约为20%，耐水性约为重量损失的2%，体外粘附性良好。此外，还证实了其对不同 种菌株的体外抗真菌活性。AmB释放和离体渗透性研究表明，在24小时内，AmB从指甲油中释放出来并渗透到指甲基质中的比例为47.76±0.07%。总之，载有AmB的指甲油显示出自身是一种有前途的临时剂型，对甲癣具有显著的抗活性。
