Enhanced oral absorption of salmon calcitonin-encapsulated PLGA nanoparticles by adding organic substances

• Published in: The Korean journal of chemical engineering Vol. 26; no. 1; pp. 131 - 135
• Main Authors: Jung, Tae-Sung, Kwon, Byung-Soo, Lee, Hea-Eun, Kim, Ah-Young, Lee, Min-Jeong, Park, Cho-Rong, Kang, Ho-Kyung, Kim, Young-Deug, Lee, Sang-Kil, Kang, Jae-Seon, Choi, Guang-Jin
• Format: Journal Article
• Language: English
• Published: Boston Springer US 01.01.2009; 한국화학공학회
• Subjects: Biotechnology; Catalysis; Chemistry; Chemistry and Materials Science; Environmental Engineering; Industrial Chemistry/Chemical Engineering; Materials Science; 화학공학; Encapsulation; Bile Acid; Transferrin; Salmon Calcitonin; PLGA, Absorption Enhancer; Poly(lactide-co-glycolide); Oral Delivery
• ISSN: 0256-1115; 1975-7220
• DOI: 10.1007/s11814-009-0020-2

Two organic compounds with potential absorption enhancing effects, bile acids and transferrin, were examined by the gastro-intestinal (GI) absorption of therapeutic salmon calcitonin (sCT) as encapsulated by poly(lactide-co-glycolide) (PLGA) for the treatment of osteoporosis. The sCT-loaded PLGA nanocapsules were prepared by O/W emulsification approach. Either additive of a designated content was mixed with sCT dissolved in methanol. For bile acids, their content (0–7.5 mg to sCT 6 mg) was observed to have a substantial effect both on the emulsification process and the encapsulation efficiency. When 1.5 mg of bile acids was added, sCT-loaded PLGA nanocapsules of about 700 nm in diameter and with a fairly high encapsulation efficiency greater than 35% were produced. Accordingly, this formulation gave the most significant hypocalcemic effect in an in vivo experiment with SD rats. On the other hand, a too high bile acids loading resulted in a poor encapsulation efficiency of less than 7%. Two principal roles of bile acids were proposed: emulsifying agent and absorption enhancer. Transferrin, a human glycoprotein of 80 kDa molecular weight, turned out to have potential as absorption enhancer as well.