PLGA from PolySciTech used in development of oral microparticles for localized colon delivery of 5FU as colorectal cancer treatment

 

Under normal oral drug delivery conditions, it is desired for the medicine to be released in the small intestine, or before if it is stable in acid, and to uptake across the lumen into the bloodstream. However, for treating issues located in the colorectal area, better drug delivery is achieved by designing a formulation which delays release beyond the small intestine and delivers the drug directly into the large intestine and colorectal area. This can be utilized to achieve localized delivery to a portion of the body which is not normally the target for localized delivery. Researchers at Pusan National University and Korea University utilized PLGA (AP037) from PolySciTech Division of Akina, Inc. (www.polyscitech.com) to develop chemotherapeutic, 5-FU, loaded microparticles designed to pass through the stomach and intestines before releasing the drug into the colon for targeted treatment of colorectal cancer. This research holds promise to provide for improved treatment against cancer. Read more: Lee, Juho, Junhwan Bae, Dongmin Kwak, Hyunwoo Kim, Jihyun Kim, Shwe Phyu Hlaing, Aruzhan Saparbayeva et al. "5-Fluorouracil crystal-incorporated, pH-responsive, and release-modulating PLGA/Eudragit FS hybrid microparticles for local colorectal cancer-targeted chemotherapy." International Journal of Pharmaceutics (2022): 122443. https://www.sciencedirect.com/science/article/pii/S037851732200998X

“Abstract: 5-Fluorouracil (5-FU) is a widely used chemotherapeutic agent for colorectal cancer (CRC) owing to its potent anticancer effects. However, severe systemic side effects and poor drug accumulation in the CRC tissues limit its efficacy. This study aimed to develop 5-FU crystal-incorporated, pH-responsive, and release-modulating poly(d,l-lactide-co-glycolide)/Eudragit FS hybrid microparticles (5FU-EPMPs) for the local CRC-targeted chemotherapy. Approximately 150 μm 5FU-EPMPs were fabricated via the S/O/W emulsion solvent evaporation method, with 7.93 ± 0.24% and 87.23 ± 2.64% 5-FU loading and encapsulation efficiencies, respectively. Drug release profiles in a simulated pH environment of the gastrointestinal tract revealed that premature 5-FU release in the stomach and small intestine was prevented, thereby minimizing systemic 5-FU absorption. After reaching the colon, 5-FU was continuously released for >15 h, allowing long-term exposure of CRC tissues to sufficient 5-FU concentrations. Furthermore, in a CRC mouse model, the 5FU-EPMPs showed potent inhibition of tumor growth without signs of systemic toxicity. Thus, the 5FU-EPMPs represent a promising drug delivery system for local CRC-targeted chemotherapy. Keywords: 5-fluorouracil pH-responsive release modulation colorectal cancer colon-targeted delivery local chemotherapy.”