Mannosylated imiquimod-terbinafine co-loaded transethosomes for cutaneous leishmaniasis
- Title
- Mannosylated imiquimod-terbinafine co-loaded transethosomes for cutaneous leishmaniasis
- Author
- 최한곤
- Keywords
- Anti-leishmanial; Nano transethosomes; Mannosylated transethosomal gel; Imiquimod; Terbinafine
- Issue Date
- 2022-12-22
- Publisher
- ELSEVIER
- Citation
- BIOMATERIALS ADVANCES
- Abstract
- Current treatment options for cutaneous leishmaniasis are associated with myriad limiting factors including low penetration, poor efficacy, and drug toxicities. Herein, we reported imiquimod and terbinafine co-loaded mannosylated transethosomes (IMQ-TER-MTES) with enhanced cutaneous retention, macrophage targeting, antileishmanial potential, and dermal mmunomodulation. IMQ-TER-MTES were optimized using Design Expert® followed by their loading into chitosan gel. Moreover, the antileishmanial response against amastigotes-infected macrophages and Leishmania-infected BALB/c mice was evaluated. Finally, the safety and immunomodulation activity of IMQ-TER-MTES gel was performed using BALB/c mice. Optimized IMQ-TER-MTES showed nano-sized particles with low poly-dispersibility index (PDI) and high drug entrapment. Mannosylation has augmented macrophage targeting and the internalization capability of TES. IMQ-TER-MTES showed significantly reduced IC50 value (19.56 ± 3.62 μg/ml), higher selectivity index (29.24), and synergism against Leishmania major
(L. major) amastigotes. In L. major infected BALB/c mice, the cutaneous lesion healing potential of IMQ-TERMTES was also elevated with reduced lesion size (1.52 ± 0.43 mm). Superior safety of IMQ-TER-MTES was observed in BALB/c mice along with adequate stimulation of dermal immune cells, in contrast to the ALDARA®. Moreover, incremented Nuclear factor Kappa-β (NF-κβ) and nitric oxide (NO) biosynthesis were observed with IMQ-TER-MTES.
- URI
- https://information.hanyang.ac.kr/#/eds/detail?an=S277295082200543X&dbId=edselphttps://repository.hanyang.ac.kr/handle/20.500.11754/189770
- ISSN
- 2772-9508
- DOI
- 10.1016/j.bioadv.2022.213266
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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