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Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study

1
School of Pharmacy, Medical Biology Centre, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK
2
Department of Pharmaceutics, Faculty of Pharmacy, Hasanuddin University, Makassar 90234, Indonesia
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(7), 346; https://doi.org/10.3390/pharmaceutics11070346
Received: 25 June 2019 / Revised: 10 July 2019 / Accepted: 13 July 2019 / Published: 17 July 2019
(This article belongs to the Special Issue Drug Delivery Systems Using Various Microneedle Technologies)
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Abstract

Conventional oral administration of antifilariasis drugs results in nonspecific targeting of the drugs and the intradermal delivery of nanoparticles with sizes of <100 nm could be used to improve lymphatic uptake. This study investigated the combination of nanosuspension and dissolving microneedles (MN-NS) as an alternative intradermal delivery approach for the delivery of antifilariasis drugs, namely doxycycline, albendazole, and ivermectin. NS were fabricated and optimized using a bottom-up technique. The NS were then incorporated into the MN arrays. The optimized NS were <100 nm in diameter. Furthermore, MN-NS had suitable mechanical strength and insertion capabilities. The dermatokinetic study revealed that the delivery of drugs into the dermis of excised neonatal porcine skin by MNs was significantly higher than that from a needle-free patch, with 29.29 ± 4.65%, 31.54 ± 5.35%, and 34.54 ± 4.98% of doxycycline, albendazole sulfoxide, and ivermectin retained in the dermis after 24 h. The results presented here serve as proof of concept for the significant enhancement of drug retention times in the dermis, following their formulation into NS and delivery via MN. Leading on from these studies, future work must investigate in vivo lymphatic pharmacokinetic profiling of drugs formulated into NS, in a suitable animal model. View Full-Text
Keywords: doxycycline; albendazole; ivermectin; nanosuspension; microneedles; dermatokinetic; lymphatic filariasis doxycycline; albendazole; ivermectin; nanosuspension; microneedles; dermatokinetic; lymphatic filariasis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Permana, A.D.; McCrudden, M.T.C.; Donnelly, R.F. Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study. Pharmaceutics 2019, 11, 346.

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