Pollen grains as a novel microcarrier for oral delivery of proteins.
Pollen grains as a novel microcarrier for oral delivery of proteins.
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DOI：
10.1016/j.ijpharm.2018.10.016
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发表时间：
2018-12-01
影响因子：
5.8
通讯作者：
Gill HS
中科院分区：
文献类型：
--
作者：
Lale SV;Gill HS
蛋白质和肽的口服递送是一个挑战，因为它们在胃中降解。为了克服这一挑战，豚草（豚草）花粉粒被改造为保护性微胶囊。将由Eudragit L100-55（一种肠溶聚合物）组成的基质沉积在豚草花粉的内表面上，以保护包封的蛋白质免于胃降解并实现肠中的pH依赖性释放。在不使用有机溶剂的情况下形成Eudragit L100-55基质，从而可以防止溶剂诱导的对蛋白质分子的损伤。为了证明这一概念，使用了牛血清白蛋白（BSA）模型蛋白。通过优化豚草花粉各自的浓度以最大化BSA在基质中的负载量，在豚草花粉中制备包埋有BSA的Eudragit L100-55基质。在模拟胃酸溶液中考察了该优化处方对牛血清白蛋白的保护作用。在模拟胃液（pH 1.2）中的释放研究显示从豚草-Eudragit L100-55制剂释放最小的BSA。对暴露于胃液后保留在制剂中的BSA进行分析，证实残留BSA未变性。在模拟肠液（pH 6.8）中的释放研究表明，豚草花粉提供了额外的控制释放机制，在最初的几个小时内释放凭借其固体壁。总之，在使用Eudragit L100-55的蛋白质友好溶剂时，蛋白质可以包封在豚草花粉中而不使其变性，并且所得制剂在肠道pH下表现出蛋白质的选择性释放，这表明基于豚草花粉粒的制剂可能有希望用于蛋白质的口服递送。
Oral delivery of proteins and peptides is a challenge due to their degradation in the stomach. To overcome this challenge, ragweed (Ambrosia elatior) pollen grains were engineered to serve as protective microcapsules. A matrix comprising of Eudragit L100-55, an enteric polymer was deposited on the inner surfaces of ragweed pollens to protect the encapsulated protein from gastric degradation and to achieve pH-dependent release in the intestine. The Eudragit L100-55 matrix was formed without use of organic solvents so that solvent-induced damage to protein molecules could be prevented. To demonstrate the concept, bovine serum albumin (BSA) a model protein was used. A matrix of Eudragit L100-55 embedded with BSA was prepared in ragweed pollens by optimizing their respective concentrations for maximizing BSA loading in the matrix. The ability of this optimized formulation to protect BSA in simulated gastric acid fluid was evaluated. Release studies in simulated gastric fluid (pH 1.2) showed minimal BSA release from the ragweed-Eudragit L100-55 formulation. Analysis of BSA retained in the formulation after its exposure to gastric fluid confirmed that the residual BSA had not denatured. Release studies in the simulated intestinal fluid (pH 6.8) showed that ragweed pollen offered additional controlled release mechanism within the first few hours of release by virtue of their solid wall. In conclusion, upon use of a protein-friendly solvent for Eudragit L100-55, proteins could be encapsulated in ragweed pollen without denaturing them, and the resulting formulation exhibited selective release of the proteins at intestinal pH suggesting that the ragweed pollen grain-based formulation could be promising for oral delivery of proteins.
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