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Preparation and characterization of genipin-cross-linked silk fibroin/chitosan sustained-release microspheres.
Drug Des Devel Ther. 2015; 9:2501-14.DD

Abstract

We report the effects of distinct concentrations of genipin and silk fibroin (SF):chitosan (CS) ratios on the formation of SF-CS composite microspheres. We selected microspheres featuring an SF:CS ratio of 1:1, encapsulated various concentrations of bovine serum albumin (BSA), and then compared their encapsulation efficiency and sustained-release rate with those of pure CS microspheres. We determined that the following five groups of microspheres were highly spherical and featured particle sizes ranging from 70 μm to 147 μm: mass ratio of CS:SF =1:0.5, 0.1 g or 0.5 g genipin; CS:SF =1:1, 0.05 g or 1 g genipin; and CS:SF =1:2, 0.5 g genipin. The microspheres prepared using 1:1 CS:SF ratio and 0.05 g genipin in the presence of 10 mg, 20 mg, and 50 mg of BSA exhibited encapsulation efficiencies of 50.16%±4.32%, 56.58%±3.58%, and 42.19%±7.47%, respectively. Fourier-transform infrared spectroscopy (FTIR) results showed that SF and CS were cross-linked and that the α-helices and random coils of SF were converted into β-sheets. BSA did not chemically react with CS or SF. Moreover, thermal gravimetric analysis (TGA) results showed that the melting point of BSA did not change, which confirmed the FTIR results, and X-ray diffraction results showed that BSA was entrapped in microspheres in a noncrystalline form, which further verified the TGA and FTIR data. The sustained-release microspheres prepared in the presence of 10 mg, 20 mg, and 50 mg of BSA burst release 30.79%±3.43%, 34.41%±4.46%, and 41.75%±0.96% of the entrapped BSA on the 1st day and cumulatively released 75.20%±2.52%, 79.16%±4.31%, and 89.04%±4.68% in 21 days, respectively. The pure CS microspheres prepared in the presence of 10 mg of BSA burst release 39.53%±1.76% of BSA on the 1st day and cumulatively released 83.57%±2.33% of the total encapsulated BSA in 21 days. The SF-CS composite microspheres exhibited higher sustained release than did the pure CS microspheres, and thus these composite microspheres might function as a superior drug carrier.

Authors+Show Affiliations

Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, Guangdong, People's Republic of China.Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, Guangdong, People's Republic of China ; Department of Stomatology, Guangdong Women and Children Hospital, Guangzhou Medical University, Guangzhou, Guangdong, People's Republic of China.Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, Guangdong, People's Republic of China.Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, Guangdong, People's Republic of China.Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, Guangdong, People's Republic of China.Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, Guangdong, People's Republic of China.Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, Guangdong, People's Republic of China.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

25999693

Citation

Zeng, Shuguang, et al. "Preparation and Characterization of Genipin-cross-linked Silk Fibroin/chitosan Sustained-release Microspheres." Drug Design, Development and Therapy, vol. 9, 2015, pp. 2501-14.
Zeng S, Ye M, Qiu J, et al. Preparation and characterization of genipin-cross-linked silk fibroin/chitosan sustained-release microspheres. Drug Des Devel Ther. 2015;9:2501-14.
Zeng, S., Ye, M., Qiu, J., Fang, W., Rong, M., Guo, Z., & Gao, W. (2015). Preparation and characterization of genipin-cross-linked silk fibroin/chitosan sustained-release microspheres. Drug Design, Development and Therapy, 9, 2501-14. https://doi.org/10.2147/DDDT.S78402
Zeng S, et al. Preparation and Characterization of Genipin-cross-linked Silk Fibroin/chitosan Sustained-release Microspheres. Drug Des Devel Ther. 2015;9:2501-14. PubMed PMID: 25999693.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and characterization of genipin-cross-linked silk fibroin/chitosan sustained-release microspheres. AU - Zeng,Shuguang, AU - Ye,Manwen, AU - Qiu,Junqi, AU - Fang,Wei, AU - Rong,Mingdeng, AU - Guo,Zehong, AU - Gao,Wenfen, Y1 - 2015/05/04/ PY - 2015/5/23/entrez PY - 2015/5/23/pubmed PY - 2016/2/3/medline KW - chitosan KW - controlled release KW - genipin KW - microspheres KW - silk fibroin SP - 2501 EP - 14 JF - Drug design, development and therapy JO - Drug Des Devel Ther VL - 9 N2 - We report the effects of distinct concentrations of genipin and silk fibroin (SF):chitosan (CS) ratios on the formation of SF-CS composite microspheres. We selected microspheres featuring an SF:CS ratio of 1:1, encapsulated various concentrations of bovine serum albumin (BSA), and then compared their encapsulation efficiency and sustained-release rate with those of pure CS microspheres. We determined that the following five groups of microspheres were highly spherical and featured particle sizes ranging from 70 μm to 147 μm: mass ratio of CS:SF =1:0.5, 0.1 g or 0.5 g genipin; CS:SF =1:1, 0.05 g or 1 g genipin; and CS:SF =1:2, 0.5 g genipin. The microspheres prepared using 1:1 CS:SF ratio and 0.05 g genipin in the presence of 10 mg, 20 mg, and 50 mg of BSA exhibited encapsulation efficiencies of 50.16%±4.32%, 56.58%±3.58%, and 42.19%±7.47%, respectively. Fourier-transform infrared spectroscopy (FTIR) results showed that SF and CS were cross-linked and that the α-helices and random coils of SF were converted into β-sheets. BSA did not chemically react with CS or SF. Moreover, thermal gravimetric analysis (TGA) results showed that the melting point of BSA did not change, which confirmed the FTIR results, and X-ray diffraction results showed that BSA was entrapped in microspheres in a noncrystalline form, which further verified the TGA and FTIR data. The sustained-release microspheres prepared in the presence of 10 mg, 20 mg, and 50 mg of BSA burst release 30.79%±3.43%, 34.41%±4.46%, and 41.75%±0.96% of the entrapped BSA on the 1st day and cumulatively released 75.20%±2.52%, 79.16%±4.31%, and 89.04%±4.68% in 21 days, respectively. The pure CS microspheres prepared in the presence of 10 mg of BSA burst release 39.53%±1.76% of BSA on the 1st day and cumulatively released 83.57%±2.33% of the total encapsulated BSA in 21 days. The SF-CS composite microspheres exhibited higher sustained release than did the pure CS microspheres, and thus these composite microspheres might function as a superior drug carrier. SN - 1177-8881 UR - https://www.unboundmedicine.com/medline/citation/25999693/Preparation_and_characterization_of_genipin_cross_linked_silk_fibroin/chitosan_sustained_release_microspheres_ L2 - https://dx.doi.org/10.2147/DDDT.S78402 DB - PRIME DP - Unbound Medicine ER -