MODERNIZING A THAI TRADITIONAL REMEDY: IN VITRO-EX VIVO AND BIOACTIVITY PERFORMANCE OF CLOTRIMAZOLE-EMBEDDED IN SITU FORMING PAINT
DOI:
https://doi.org/10.55766/sujst10797Keywords:
Bioactivity, Clotrimazole, In situ Forming Paint, Performance, PermeationAbstract
“Ya-Pai,” a traditional Thai powdered medicine applied as an oral paint, presents application challenges and has seen limited formulation development. This study aims to modernize Ya-Pai by developing it into an advanced dosage form, an in situ forming system, for the treatment of oropharyngeal candidiasis (OPC). Clotrimazole-embedded in situ forming paints (ISPs) were developed using lauric acid and palmitic acid as ISP formers for the treatment of OPC. Their formation of matrix layer, transformation at interface, buccal mucosa permeation, and antifungal activities investigated to prove the concept. The formulation with a high concentration of ISP former (F2) demonstrated superior matrix formation and a rapid transition at the interface within 0.5 minutes, along with slower matrix growth compared to other formulations (5 minutes). In contrast, the formulation with a low concentration of ISP former (F1) exhibited faster drug permeation through the buccal mucosa and a lower percentage of drug remaining in the buccal mucosa (28.64 ± 2.80 % and 20.27 ± 1.27 % for F2 and F1, respectively). The drug permeation rates of F1 and F2 were 4.0363%/hour1/2 and 3.492%/hour1/2, respectively, following Higuchi’s model. The antifungal test using the agar diffusion method demonstrated that the prepared ISPs effectively inhibited the growth of Candida albicans (32.3 ± 0.6 and 29.3 ± 1.2 mm for F1 and F2, respectively) and others. Thereby, the developed clotrimazole-embedded ISP shows a promising concept as a modernized Ya-Pai for the OPC treatment. However, further study such as in vivo efficacy, mucosal safety, and pharmacokinetic evaluation should be conducted.
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