A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery

Transepidermal drug delivery achieves high drug concentrations at the action site and ensures continuous drug delivery and better patient compliance with fewer adverse effects. However, drug delivery through topical application is still limited in terms of drug penetration. Chitosan is a promising e...

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Main Authors: Jin Sil Lee, Hyeryeon Oh, Sunghyun Kim, Jeung-Hoon Lee, Yong Chul Shin, Won Il Choi
Format: Article
Language:English
Published: MDPI AG 2021-08-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/13/9/1329
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author Jin Sil Lee
Hyeryeon Oh
Sunghyun Kim
Jeung-Hoon Lee
Yong Chul Shin
Won Il Choi
author_facet Jin Sil Lee
Hyeryeon Oh
Sunghyun Kim
Jeung-Hoon Lee
Yong Chul Shin
Won Il Choi
author_sort Jin Sil Lee
collection DOAJ
description Transepidermal drug delivery achieves high drug concentrations at the action site and ensures continuous drug delivery and better patient compliance with fewer adverse effects. However, drug delivery through topical application is still limited in terms of drug penetration. Chitosan is a promising enhancer to overcome this constraint, as it can enhance drug diffusion by opening the tight junctions of the stratum corneum. Therefore, here, we developed a novel chitosan nanosponge (CNS) with an optimal ratio and molecular weight of chitosan to improve drug penetration through skin. To prepare the CNS, two types of chitosan (3 and 10 kDa) were each conjugated with poloxamer 407 using para-nitrophenyl chloroformate, and the products were mixed with poloxamer 407 at ratios of 5:5, 8:2, and 10:0. The resulting mixtures were molded to produce flexible soft nanosponges by simple nanoprecipitation. The CNSs were highly stable in biological buffer for four weeks and showed no toxicity in human dermal fibroblasts. The CNSs increased drug permeability through human cadaver skin in a Franz-type diffusion cell, with substantially higher permeability with 3 kDa chitosan at a ratio of 8:2. This suggests the applicability of the novel CNS as a promising carrier for efficient transepidermal drug delivery.
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spelling doaj.art-97484afcc0474175835e88fee81272ab2023-11-22T14:45:59ZengMDPI AGPharmaceutics1999-49232021-08-01139132910.3390/pharmaceutics13091329A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug DeliveryJin Sil Lee0Hyeryeon Oh1Sunghyun Kim2Jeung-Hoon Lee3Yong Chul Shin4Won Il Choi5Center for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaSKINMED Co., Ltd., Daejeon 34028, KoreaSKINMED Co., Ltd., Daejeon 34028, KoreaCenter for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaTransepidermal drug delivery achieves high drug concentrations at the action site and ensures continuous drug delivery and better patient compliance with fewer adverse effects. However, drug delivery through topical application is still limited in terms of drug penetration. Chitosan is a promising enhancer to overcome this constraint, as it can enhance drug diffusion by opening the tight junctions of the stratum corneum. Therefore, here, we developed a novel chitosan nanosponge (CNS) with an optimal ratio and molecular weight of chitosan to improve drug penetration through skin. To prepare the CNS, two types of chitosan (3 and 10 kDa) were each conjugated with poloxamer 407 using para-nitrophenyl chloroformate, and the products were mixed with poloxamer 407 at ratios of 5:5, 8:2, and 10:0. The resulting mixtures were molded to produce flexible soft nanosponges by simple nanoprecipitation. The CNSs were highly stable in biological buffer for four weeks and showed no toxicity in human dermal fibroblasts. The CNSs increased drug permeability through human cadaver skin in a Franz-type diffusion cell, with substantially higher permeability with 3 kDa chitosan at a ratio of 8:2. This suggests the applicability of the novel CNS as a promising carrier for efficient transepidermal drug delivery.https://www.mdpi.com/1999-4923/13/9/1329chitosanpoloxamernanospongeskin permeationmodel drug
spellingShingle Jin Sil Lee
Hyeryeon Oh
Sunghyun Kim
Jeung-Hoon Lee
Yong Chul Shin
Won Il Choi
A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery
Pharmaceutics
chitosan
poloxamer
nanosponge
skin permeation
model drug
title A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery
title_full A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery
title_fullStr A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery
title_full_unstemmed A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery
title_short A Novel Chitosan Nanosponge as a Vehicle for Transepidermal Drug Delivery
title_sort novel chitosan nanosponge as a vehicle for transepidermal drug delivery
topic chitosan
poloxamer
nanosponge
skin permeation
model drug
url https://www.mdpi.com/1999-4923/13/9/1329
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