Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 605, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2021.120829
Keywords
Levamisole; D-optimal mixture design; Microemulsion-based gel; Alginate-boronic acid gel; Transdermal delivery
Categories
Funding
- National Natural Science Foundation of China [82003663]
- Science and Technology Agency of Fujian Province, China [2019 J01302, 2015Y4005]
- Joint Funds for the innovation of science and Technology, Fujian province [2019Y9006]
- Startup Fund for scientific research, Fujian Medical University [2018QH1011]
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The study prepared a highly malleable microemulsion-based gel for transdermal delivery of levamisole, which showed superior transdermal permeation and bioavailability in ex vivo and in vivo investigations compared to traditional gel formulations.
The objective of the present study was to prepare and evaluate a microemulsion-based hydrogel with high malleability as a transdermal delivery carrier for levamisole (LMS). A pseudo-ternary phase diagram and Doptimal mixture design were utilized to screen and optimize the microemulsion, and the formulation comprised 7.5% Maisine(TM)35-1, 33% Smix and 59.5% water. The microemulsion was physically stable with an average size of 19.3 +/- 0.1 nm and zeta potential of -3.84 +/- 0.05 mV. Moreover, a highly malleable alginate-boronic acid (alginate-BA) gel was prepared and could come into close contact with highly curved skin. The optimized microemulsion was loaded into alginate-BA gel and subjected to ex vivo and in vivo investigation. The microemulsion-based gel had desirable characterization, good stability and negligible skin irritation. The results of ex vivo permeation study showed that LMS achieved a significantly higher cumulative amount from the LMSloaded microemulsion-based gel than that from the LMS-gel. The pharmacokinetic study showed a twofold increase in relative bioavailability compared to the commercial liniment. These results provide insight into the capability of the developed malleable microemulsion-based gel to enhance the transdermal permeation and bioavailability of LMS.
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