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Ultra deformable vesicles for boosting transdermal delivery of 2-arylpropionic acid class drug for management of musculoskeletal pain

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Abstract

Purpose

The aim of this investigation was to formulate and evaluate naproxen transethosomal gel for sustained transdermal delivery for the management of musculoskeletal pain.

Methods

In this examination naproxen sodium-loaded transethosomes were developed by ethanol injection method. A 9 run, 2-factor, 3-level factorial design was used to optimize naproxen-transethosomes. Transethosomal formulations were then incorporated into hydrogel made of gelling agent carbopol 940. The formulated transethosomes were characterized for particle size, entrapment efficiency, zeta potential, in-vitro release, ex-vivo drug permeation study, drug deposition study, and in-vivo anti-inflammatory study.

Results

The results exhibited that the particle size were in the range of 56.94 ± 0.12 nm to 291.7 ± 0.09 nm. The transethosomes had higher entrapment efficiency in between 66.23 ± 1.52 and 93.11 ± 0.96% and exhibited a spherical morphology when examined by TEM analysis. The in-vitro skin permeation study carried out on rat skin exhibited enhanced skin deposition with lesser systemic absorption. The in-vivo studies carried out on rats showed the superiority of naproxen transethosomal gel in reducing the edema rate.

Conclusion

The results obtained all together demonstrated that the formulated transethosomal gel possessed a smaller particle size, high entrapment efficiency along higher skin deposition rate which is required in getting relief from musculoskeletal pain. The developed formulation could be regarded as an ideal substitute for the conventional gel for the management of musculoskeletal pain.

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Correspondence to Shreya Kaul.

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All authors (S. Kaul, N. Jain, and U. Nagaich) declare no conflicts of interest.

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The study was reviewed and approved by the Institutional Animal Ethical Committee with registration number 1327/PO/ ReBi/S/10 /CPCSEA. All institutional and national guidelines for the care and use of laboratory animals were followed.

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Kaul, S., Jain, N. & Nagaich, U. Ultra deformable vesicles for boosting transdermal delivery of 2-arylpropionic acid class drug for management of musculoskeletal pain. J. Pharm. Investig. 52, 217–231 (2022). https://doi.org/10.1007/s40005-021-00555-7

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