Oral bioavailability of a drug molecule requires its effective delivery to the target site. In general, majority of synthetically developed molecular entities have high hydrophobic nature as well as low bioavailability, therefore the need for suitable delivery vehicles arises. Self-assembled structures such as micelles, niosomes, and liposomes have been used as effective delivery vehicles and studied extensively. However, the information available in literature is mostly qualitative in nature. We have quantitatively investigated the partitioning of antibiotic drug streptomycin into cationic, nonionic, and a mixture of cationic and nonionic surfactant micelles and its interaction with the transport protein serum albumin upon subsequent delivery. A combination of calorimetry and spectroscopy has been used to obtain the thermodynamic signatures associated with partitioning and interaction with the protein and the resulting conformational changes in the latter. The results have been correlated with other class of drugs of different nature to understand the role of molecular features in the partitioning process. These studies are oriented toward understanding the physical chemistry of partitioning of a variety of drug molecules into suitable delivery vehicles and hence establishing structure–property-energetics relationships. Such studies provide general guidelines toward a broader goal of rational drug design.

中文翻译：

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胶束介质中的药物分配及其在合理药物设计中的意义：链霉素的见解

药物分子的口服生物利用度需要将其有效递送到目标部位。通常，大多数合成开发的分子实体具有高疏水性以及低生物利用度，因此出现了对合适的递送载体的需求。自组装结构，如胶束，脂质体和脂质体，已被用作有效的载体，并进行了广泛的研究。但是，文献中可用的信息本质上大多是定性的。我们已经定量研究了抗生素药物链霉素在阳离子，非离子以及阳离子和非离子表面活性剂胶束的混合物中的分配及其在后续递送时与转运蛋白血清白蛋白的相互作用。量热法和光谱法的结合已被用于获得与蛋白质的分配和相互作用以及在蛋白质中产生的构象变化有关的热力学特征。该结果已与其他不同性质的药物相关联，以了解分子特征在分配过程中的作用。这些研究的目的是理解将各种药物分子分配到合适的载体中的物理化学，从而建立结构-性质-能量学关系。这些研究为实现合理药物设计的更广泛目标提供了一般指导。该结果已与其他不同性质的药物相关联，以了解分子特征在分配过程中的作用。这些研究的目的是理解将各种药物分子分配到合适的载体中的物理化学，从而建立结构-性质-能量学关系。这些研究为实现合理药物设计的更广泛目标提供了一般指导。该结果已与其他不同性质的药物相关联，以了解分子特征在分配过程中的作用。这些研究的目的是理解将各种药物分子分配到合适的载体中的物理化学，从而建立结构-性质-能量学关系。这些研究为实现合理药物设计的更广泛目标提供了一般指导。