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J. Control. Release, Nov 30 2023, 365 S0168-3659(23)00671-5 | https://doi.org/10.1016/j.jconrel.2023.10.021 Mucoadhesive chitosan microcapsules for controlled gastrointestinal delivery and oral bioavailability enhancement of low molecular weight peptides

Kyungjik Yang ^a,1, Hwa Seung Han ^c,1, Seung Hwan An ^a, Kyung Hoon Park ^a, Keonwook Nam ^a, Shinha Hwang ^a, Yuyeon Lee ^b, Sung Yeon Cho ^b, Taehyung Kim ^a, Deokyeong Choe ^d, Sang Won Kim^e, Wonkyu Yu ^e, Hyunah Lee ^f, Jiyong Park^g, SangGuan You ^c,k, Dong-Gyu Jo ^h,i,j, Ki Young Choi ^c, Young Hoon Roh ^a,b, Jae Hyung Park ^i,j,l

^aDepartment of Biotechnology, College of Life Science and Biotechnology, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea

^bGraduate Program in Bioindustrial Engineering, College of Life Science and Biotechnology, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea

^cDepartment of Marine Food Science and Technology, Gangneung-Wonju National University, Gangneung 120, Republic of Korea

^dSchool of Food Science and Biotechnology, College of Agriculture and Life Sciences, Kyungpook National University, Daegu 41566, Republic of Korea

^eYonsei University Dairy R&D Center, Asan, Republic of Korea

^fDepartment of Bio-Convergence Engineering, Dongyang Mirae University, 445-8, Gyeongin-ro, Guro-gu, Seoul 02841, Republic of Korea

^gNutrex Technology, 670 Daewangpangyo-ro, Seongnam 13494, Republic of Korea

^hSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea

ⁱDepartment of Health Sciences and Technology, SAIHST, Sungkyunkwan University, Seoul 06351, Republic of Korea

^jBiomedical Institute for Convergence at SKKU (BICS), Sungkyunkwan University, Suwon 16419, Republic of Korea

^kEast Coast Research Institute of Life Science, Gangneung-Wonju National University, 120 Gangneung, Gangwon 210-702, Republic of Korea

^lSchool of Chemical Engineering, Sungkyunkwan University, Suwon 16419, Republic of Korea

¹These authors contributed equally to this work.

Correspondence to: D-G Jo, Ki Young Choi, Young Hoon Roh, Jae Hyung Park

Abstract

A bioactive compound, collagen peptide (CP), is widely used for biological activities such as anti-photoaging and antioxidant effects, with increased oral bioavailability because of its low molecular weight and high hydrophilicity. However, controlling release time and increasing retention time in the digestive tract for a more convenient oral administration is still a challenge. We developed CP-loaded chitosan (CS) microcapsules via strong and rapid ionic gelation using a highly negative phytic acid (PA) crosslinker. The platform enhanced the oral bioavailability of CP with controlled gastrointestinal delivery by utilizing the mucoadhesiveness and tight junction-opening properties of CS. CS and CP concentrations varied from 1.5 to 3.5% and 0-30%, respectively, for optimal and stable microcapsule synthesis. The physicochemical properties, in vitro release profile with intestinal permeability, in vivo oral bioavailability, in vivo biodistribution, anti-photoaging effect, and antioxidant effect of optimized CS microcapsules were analyzed to investigate the impact of controlling parameters. The structure of CS microcapsules was tuned by PA diffused gradient ionic cross-linking degree, resulting in a controlled CP release region in the gastrointestinal tract. The optimized microcapsules increased C _max, AUC, and t _max by 1.5-, 3.4-, and 8.0-fold, respectively. Furthermore, CP in microcapsules showed anti-photoaging effects by downregulating matrix metalloproteinases-1 via antioxidant effects. According to our knowledge, this is the first study to microencapsulate CP for oral bioavailability enhancement. The peptide delivery method employed is simple, economical, and can be applied to customize bioactive compound administration.

논문정보

형식Research article
게재일2023년 11월 (BRIC 등록일 2023-12-07)
연구진국내 연구진
분야 바이오·의료융합 > 바이오센싱 및 나노바이오물질

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