2017-07-012024-05-14https://scholars.lib.ntu.edu.tw/handle/123456789/656466摘要：對於長期服用型式來說，口服攝取一般最為大眾所接受。儘管腸胃道之吸收機制仍不明朗，但生物活性物質的生物可利用性會由於其化學結構的變化有所不同，進而影響其吸收、代謝和排泄速率。以親脂性化合物為例，在水性環境中難以溶解，因此於小腸黏膜處吸收率差。由於生物活性物質所能提供治療或生理效益之有效性大大取決於關鍵活性成分對目標作用部位的生物可利用性，因此目前研究對於能夠提高口服生物可利用性之遞送系統為主要開發重點。諸如水溶性差、停留腸胃道時間不足、生理環境改變導致之不穩定性、腸內遞送係數低、代謝轉化快等因素，會顯著降低生物活性物質對疾病預防的療效。磷脂質含有兩親性化學結構，當其在水中時會以各種方式組合，在大多數情況下會形成球形微粒，其中疏水端排列在內而親水端排列在外。這些獨特的功能使磷脂質最為適合用作賦形劑，可用於水溶性較差或是親水性的化合物。因此，在本項目此一部分，我們旨在開發以磷脂質為主要成分的各種形式之口服遞送系統。此系統包括脂質體、植物化合素、乳液和微粒，可以針對選定的生物活性物質進行研究和最適化。較佳配方之選定將取決於細胞所吸收的囊封化合物之濃度，將使用該聯合研究項目開發的細胞成像平台進行評估。 <br> Abstract: For chronic intake, oral ingestion is the favored route for consumer. Even though the GI absorption mechanism remains unclear, the bioavailability of bioactive compounds differs from one to another due to variations in their chemical structures, which effect their rate and extend of absorption, metabolism and excretion. Lipophilic compounds, for instance, are poorly soluble in the aqueous environment and, thus, are poorly taken by the intestinal lining. Significant efforts have been put into the development of delivery systems to improve the oral bioavailability. Since the effectiveness of bioactive compounds to provide therapeutic or physiological benefits greatly depends on the bioavailability of key active ingredients to the target site of action. Factors, such as poor aqueous solubility, insufficient residence time in the GI tract, instability to changing physiological environments, low transport coefficient across the intestinal lining, susceptibility to rapid metabolic transformation etc. could significantly lower the efficacy of bioactives for disease prevention. Phospholipids contain an amphiphilic chemical structure, which assembles in various ways when place in water. Most often, they form spherical micelles with the hydrophobic tails lined up pointing inward and the hydrophilic head-group pointing outward to the water, or vice versa. These unique features make phospholipids most suitable to be used as excipients not only for poorly aqueous soluble compound but also those that are hydrophilic. Thus, in this part of the subproject we aim to develop various forms of oral delivery systems using phospholipid as the main ingredients. Systems includes liposome, phytosome, emulsion, and micelles may be investigated and optimized for selected bioactive compound. The selected of the better formulation will be based on the concentration of encapsulated compound absorbed by cell. This will be evaluated using the cellular imaging platform developed in this joint project.口服配方吸收磷脂質活性物質oral formulationabsorptionphospholipidbioactive compound