| DOI: 10.29090/psa.2025.04.25.4591 | Pharm Sci Asia 2025; 52(4), 506-517 |
Formulation optimization and in vitro and ex vivo evaluation of Boesenbergia rotunda extract-loaded microemulsion using experimental design modelPanatda Wittayanukullack1,2, Praneet Opanasopit1, Phuvamin Suriyaaumporn1, Worranan Rangsimawong2,*
1 Department of Industrial Pharmacy, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
2
Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmaceutical Sciences, Ubon Ratchathani University, Ubon Ratchathani, Thailand, 34190.
Boesenbergia rotunda (L.) extract is characterized by the presence of pinostrobin (PNS) as its major active component. PNS expresses several pharmacological activities such as antioxidant, anti-inflammatory, antiviral, anticancer, and anti-aromatase activities. Similar to other flavonoids, PNS has poor water solubility, resulting in low bioavailability and limiting its clinical application. These physicochemical constraints pose significant challenges for effective transdermal delivery, particularly in achieving sufficient drug penetration across the stratum corneum. To address these limitations, the development of an effective drug delivery system that can improve both the solubility and transdermal permeation of PNS is warranted. This study aimed to develop an optimized microemulsion (ME) formulation for the transdermal delivery of B. rotunda extract, focusing on PNS. Various oils, surfactants, and co-surfactants were screened, and different surfactant to co-surfactant ratios were evaluated through pseudo-ternary phase diagrams and optimized using Design Expert software. The developed ME was characterized for physical appearance, droplet size, polydispersity index (PDI), zeta potential, pH, entrapment efficiency, in vitro release and ex vivo skin permeation. For the result, the optimized formulation was with a fixed surfactant to co-surfactant ratio of 3:1. The optimized ME consisted of 63.34% Labrasol® and Transcutol®, 18.33% limonene, and 18.33% water, which the mean droplet size, PDI, zeta potential and entrapment efficiency were discovered as 156.0±0.80 nm, 0.21±0.02, 0.05±0.03 mV, and 99.79%, respectively. In vitro drug release studies demonstrated that the ME exhibited a higher release rate than the oil solution but a lower release rate than the extract in ethanol solution over a 24-hour period. Ex vivo skin permeation studies revealed that the optimized ME demonstrated significantly higher skin permeation than the control formulations. In conclusion, these findings suggest that the developed ME is a promising carrier system for enhancing the transdermal delivery of PNS.
Keyword:
Boesenbergia rotunda extract; Pinostrobin; Microemulsion; Design expert
Download full paper (PDF File size: 844.70 KB.)
|
