Complexation Hydrogels for the Oral Delivery of Growth Hormone and Salmon Calcitonin.
Complexation Hydrogels for the Oral Delivery of Growth Hormone and Salmon Calcitonin.
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DOI：
10.1021/ie1008025
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发表时间：
2010-09-29
影响因子：
4.2
通讯作者：
Peppas, Nicholas A.
中科院分区：
文献类型：
--
作者：
Carr, Daniel A.;Gomez-Burgaz, Marta;Boudes, Mathilde C.;Peppas, Nicholas A.
对聚（甲基丙烯酸-N-乙烯基吡咯烷酮）水凝胶系统作为生长激素和鲑鱼降钙素的口服给药系统进行了评估。选择这些蛋白质是因为它们的治疗重要性以及通过评估高分子量治疗剂（生长激素）和高等电点药物（鲑鱼降钙素）的递送提供的见解。对 P(MAA-co-NVP) 和 P(MAA-g-PEG) 进行生长激素加载和释放研究。各个系统的加载效率分别为 50.9 ± 1.8% 和 57.8 ± 4.1%；蛋白质的重量掺入量确定为3.5±0.1%和4.0±0.3%。在 pH 7.4 时，P(MAA-co-NVP) 微粒在 45 分钟内释放了 90% 的生长激素； P(MAA-g-PEG) 微粒直到 180 分钟才实现 90% 的释放。在pH 1.2时，P(MAA-co-NVP)微粒没有释放，但P(MAA-g-PEG)微粒释放了10%。鲑鱼降钙素的装载和释放受到去质子化 MAA 负电荷的影响；对于单体摩尔进料比为 4:1、1:1 和 1:4 MAA:NVP 的系统，加载效率确定为 70.6 ± 3.0%、25.3 ± 1.2% 和 1.6 ± 1.3%。 pH 7.4 时，含有 4:1 MAA:NVP 单体饲料的共聚物中鲑鱼降钙素的释放量最少。当 pH 值升至生理水平以上时，释放得到改善。这些研究证实 P(MAA-co-NVP) 是一种有效的高分子量药物口服递送系统，但在该系统用于高等电点治疗递送之前还需要改进。
The hydrogel system of poly(methacrylic acid-co-N-vinyl pyrrolidone) was evaluated for use as an oral delivery system for growth hormone and salmon calcitonin. These proteins were selected because of their therapeutic importance and the insight provided by evaluating the delivery of a therapeutic agent with a high molecular weight (growth hormone) and a drug with a high isoelectric point (salmon calcitonin). Growth hormone loading and release studies were performed for both P(MAA-co-NVP) and P(MAA-g-PEG). Loading efficiencies for the respective systems were 50.9 ± 1.8% and 57.8 ± 4.1%; weight incorporation of the protein was determined to be 3.5 ± 0.1% and 4.0 ± 0.3%. At pH 7.4, growth hormone release of 90% occurred within 45 min for P(MAA-co-NVP) microparticles; 90% release was not achieved with P(MAA-g-PEG) microparticles until 180 min. At pH 1.2, no release occurred from P(MAA-co-NVP) microparticles but 10% release occurred from P(MAA-g-PEG) microparticles. Salmon calcitonin loading and release were shown to be affected by the negative charges of deprotonated MAA; for systems with monomer molar feed ratios of 4:1, 1:1 and 1:4 MAA:NVP, loading efficiencies were determined to be 70.6 ± 3.0%, 25.3 ± 1.2%, and 1.6 ± 1.3%. Salmon calcitonin release was minimal from the copolymer with 4:1 MAA:NVP monomer feed at pH 7.4. The release improved when the pH was raised above physiological levels. These studies confirmed that P(MAA-co-NVP) was an effective oral delivery system for high molecular weight drugs, but improvements are needed before the system could be utilized for high isoelectric point therapeutic delivery.
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影响因子：
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发表时间：
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影响因子：
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