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Development of brucine-loaded microsphere/thermally responsive hydrogel combination system for intra-articular administration.
J Control Release. 2012 Sep 28; 162(3):628-35.JC

Abstract

Intra-articular drug delivery system could directly deliver a drug to an affected joint and offer the possibility of reaching high drug concentrations at the site of action with limited systemic toxicity. However, depending on their chemical structure, some active compounds were rapidly cleared from the joint, thus requiring numerous injections, which could cause infection or joint disability. To control the release behavior for prolonged time periods, a novel biologically based drug delivery vehicle was designed for intra-articular using microsphere/thermally responsive hydrogel combination system in this paper. And brucine was the test drug. The system was constructed by dispersing the brucine microspheres which was prepared by using a spray-drying method in a thermally responsive biopolymer hydrogel contained with chitosan-glycerol-borax. The microspheres were spherical as evidenced by the scanning electron microscopy (SEM) photographs. And the entrapment rate was 98.60% w/w with an average size range of 0.9-4.5 μm. Fourier transforms infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) revealed the absence of drug-polymer interaction and amorphous nature of an entrapped drug. From the in vitro drug release study we could see that there was a burst release of microsphere, which was obviously retarded when dispersed in hydrogel. And the studies of biocompatibility with synovium showed that no apparent thickening or hyperplasia of the synovium, a small quality of phlogocyte imbibitions was observed. The results of FX imaging in rats showed that by intra-articular injection the BMH could stay in articular for over 7 days were consistent with our in vitro release. And the results of pharmacodynamics revealed the BMH could benefit OA joint by suppressing the levels of TNF-α and IL-1β, protect the damaged joint from degradation. The novel microsphere/thermoresponsive hydrogel combination system could be a promising treatment option for OA and RA. In conclusion, the system appears to be generally biocompatible with synovium and could control the drug release for several days; hence it might be suitable for the development of treatment strategies for rheumatic diseases.

Authors+Show Affiliations

Department of Pharmacy, Nanjing University of Traditional Chinese Medicine, Nanjing 210046, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

22967750

Citation

Chen, Zhi-peng, et al. "Development of Brucine-loaded Microsphere/thermally Responsive Hydrogel Combination System for Intra-articular Administration." Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 162, no. 3, 2012, pp. 628-35.
Chen ZP, Liu W, Liu D, et al. Development of brucine-loaded microsphere/thermally responsive hydrogel combination system for intra-articular administration. J Control Release. 2012;162(3):628-35.
Chen, Z. P., Liu, W., Liu, D., Xiao, Y. Y., Chen, H. X., Chen, J., Li, W., Cai, H., Li, W., Cai, B. C., & Pan, J. (2012). Development of brucine-loaded microsphere/thermally responsive hydrogel combination system for intra-articular administration. Journal of Controlled Release : Official Journal of the Controlled Release Society, 162(3), 628-35. https://doi.org/10.1016/j.jconrel.2012.07.037
Chen ZP, et al. Development of Brucine-loaded Microsphere/thermally Responsive Hydrogel Combination System for Intra-articular Administration. J Control Release. 2012 Sep 28;162(3):628-35. PubMed PMID: 22967750.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of brucine-loaded microsphere/thermally responsive hydrogel combination system for intra-articular administration. AU - Chen,Zhi-peng, AU - Liu,Wen, AU - Liu,Dan, AU - Xiao,Yan-yu, AU - Chen,Hong-xuan, AU - Chen,Jun, AU - Li,Weidong, AU - Cai,Hao, AU - Li,Wei, AU - Cai,Bao-chang, AU - Pan,Jinhuo, Y1 - 2012/08/07/ PY - 2012/01/07/received PY - 2012/06/13/revised PY - 2012/07/31/accepted PY - 2012/9/13/entrez PY - 2012/9/13/pubmed PY - 2013/2/21/medline SP - 628 EP - 35 JF - Journal of controlled release : official journal of the Controlled Release Society JO - J Control Release VL - 162 IS - 3 N2 - Intra-articular drug delivery system could directly deliver a drug to an affected joint and offer the possibility of reaching high drug concentrations at the site of action with limited systemic toxicity. However, depending on their chemical structure, some active compounds were rapidly cleared from the joint, thus requiring numerous injections, which could cause infection or joint disability. To control the release behavior for prolonged time periods, a novel biologically based drug delivery vehicle was designed for intra-articular using microsphere/thermally responsive hydrogel combination system in this paper. And brucine was the test drug. The system was constructed by dispersing the brucine microspheres which was prepared by using a spray-drying method in a thermally responsive biopolymer hydrogel contained with chitosan-glycerol-borax. The microspheres were spherical as evidenced by the scanning electron microscopy (SEM) photographs. And the entrapment rate was 98.60% w/w with an average size range of 0.9-4.5 μm. Fourier transforms infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) revealed the absence of drug-polymer interaction and amorphous nature of an entrapped drug. From the in vitro drug release study we could see that there was a burst release of microsphere, which was obviously retarded when dispersed in hydrogel. And the studies of biocompatibility with synovium showed that no apparent thickening or hyperplasia of the synovium, a small quality of phlogocyte imbibitions was observed. The results of FX imaging in rats showed that by intra-articular injection the BMH could stay in articular for over 7 days were consistent with our in vitro release. And the results of pharmacodynamics revealed the BMH could benefit OA joint by suppressing the levels of TNF-α and IL-1β, protect the damaged joint from degradation. The novel microsphere/thermoresponsive hydrogel combination system could be a promising treatment option for OA and RA. In conclusion, the system appears to be generally biocompatible with synovium and could control the drug release for several days; hence it might be suitable for the development of treatment strategies for rheumatic diseases. SN - 1873-4995 UR - https://www.unboundmedicine.com/medline/citation/22967750/Development_of_brucine_loaded_microsphere/thermally_responsive_hydrogel_combination_system_for_intra_articular_administration_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0168-3659(12)00604-9 DB - PRIME DP - Unbound Medicine ER -