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1.华北理工大学材料科学与工程学院,唐山 063210
2.华北理工大学药学院,唐山 063210
3.华北理工大学基础医学院,唐山 063210
*乔宁(1987-),女,讲师,主要从事药物共晶、药物载体材料、生物医用高分子材料研究。E-mail: qiaoning@ncst.edu.cn.
纸质出版日期:2022-08-20,
收稿日期:2021-03-09,
修回日期:2021-12-29,
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朱杰, 李琪, 王子萌, 陈旸, 高玲焕, 梁子源, 乔宁. PVP-semi-IPN-PCL/PLA 水凝胶制备及负载卡马西平药物共晶体外释放[J]. 高分子通报, 2022,35(8):47-53.
Jie ZHU, Qi LI, Zi-meng WANG, Yang CHEN, Ling-huan GAO, Zi-yuan LIANG, Ning QIAO. Preparation and
朱杰, 李琪, 王子萌, 陈旸, 高玲焕, 梁子源, 乔宁. PVP-semi-IPN-PCL/PLA 水凝胶制备及负载卡马西平药物共晶体外释放[J]. 高分子通报, 2022,35(8):47-53. DOI: 10.14028/j.cnki.1003-3726.2022.08.006.
Jie ZHU, Qi LI, Zi-meng WANG, Yang CHEN, Ling-huan GAO, Zi-yuan LIANG, Ning QIAO. Preparation and
通过
N
-乙烯基吡咯烷酮(
N
-vinyl pyrrolidone
NVP)在聚己内酯(polycaprolactone
PCL)、聚乳酸 (poly(lactic acid)
PLA)乙酸乙酯溶液中自由基聚合
制得聚乙烯吡咯烷酮(Polyvinylpyrrolidone
PVP)/聚己内酯、聚乳酸半互穿网络(semi-interpenetrating network
semi-IPN)水凝胶(PVP-semi-IPN-PCL/PLA)。实验制得疏水/亲水比例分别为1∶9、3∶7、5∶5的三种水凝胶。采用溶剂挥发法制备卡马西平-丁二酸药物共晶 (carbamazepine-succinic acid
CBZ-SUC)。使用PVP-semi-IPN-PCL/PLA 负载CBZ-SUC共晶
考察上述三种凝胶药物载体的载药能力及体外释放行为。使用1∶9、3∶7、5∶5比例凝胶制备了载药量分别为17%、19%、 21%
包封率分别为71%、83%、89%的载药凝胶
其在37℃
pH=6.8 PBS溶液中体外释放效果均优于未使用凝胶载体的CBZ-SUC共晶。其中
3∶7组载药凝胶的累积释放量最高
溶解96h时累积释放量达到约70%。实验结果表明PVP-semi-IPN-PCL/PLA 对CBZ-SUC药物共晶具有负载和控释能力
通过将药物共晶与凝胶药物载体两种手段相结合
能够抑制药物共晶的溶液介导相转变现象
为改善难溶性药物溶解行为
提高其生物利用度提供了一个有效手段。
Polyvinylpyrrolidone-semi-interpenetrating network-polycaprolactone/poly(lactic acid) (PVP-semi-IPNPCL/ PLA) hydrogels were prepared through free radical polymerization of N-vinyl pyrrolidone (NVP) in ethyl acetate solution of PCL and PLA. Three kinds of PVP-semi-IPN-PCL/PLA hydrogels were prepared with the hydrophobic to hydrophilic ratio of 1∶9
3∶7
5∶5
respectively. Carbamazepine-succinic acid (CBZ-SUC) cocrystal was prepared through evaporation method. PVP-semi-IPN-PCL/PLA hydrogels were used as drug vector for CBZ-SUC cocrystal delivery. The CBZ-SUC cocrystal loading and
in vitro
release abilities of PVP-semi-IPN-PCL/PLA hydrogels with different hydrophobic to hydrophilic ratios were studied. CBZ-SUC cocrystal loaded hydrogels were prepared with the drug loading capacity of 17%
19%
21%
encapsulation efficiency of 71%
83%
89%
respectively. The
in vitro
release of CBZ was studied in pH 6.8 PBS solution at 37℃
and the results show that the release profiles of hydrogels loaded CBZ cocrystal were better than those of CBZ cocrystal without hydrogels vector. The 3∶7 hydrogel loaded CBZ cocrystal has the highest cumulative release amount
which reached about 70% when dissolved for 96 h. The results of this study show that PVPsemi- IPN-PCL/PLA hydrogels are capable of loading and control release of CBZ-SUC cocrystal. The combination of pharmaceutical cocrystal and hydrogel drug vector can restrain the solution mediated phase transition of cocrystal
which can be an effective way to improve the dissolution behavior and bioavailability of poorly soluble drugs.
PVP-semi-IPN-PCL/PLA水凝胶药物载体药物共晶体外释放
PVP-semi-IPN-PCL/PLA hydrogelDrug vectorPharmaceutical cocrystalin vitro release
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