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文獻名： Screening of Electrolyte Complexes Formed Between Dextran Sulfate and Amine Structures of Small-Molecule Drugs

 

 

作者： Choi, Seung Ah ¹ ; Park, Eun Ji ¹ ; Kim, Young Hun ¹ ; Jee, Jun-Pil ² ; Kim, Sung-Tae ³ ; Jang, Dong-Jin ⁴ ; Min, Kyung Ah ¹ ; Cho, Kwan Hyung ¹ ; 

1: College of Pharmacy, Inje Institute of Pharmaceutical Sciences and Research, Inje University, Gimhae 50834, Republic of Korea 

2: College of Pharmacy, Chosun University, 309 Pilmun-daero, Dong-gu, Gwangju 61452, Republic of Korea 

3: Department of Pharmaceutical Engineering, Inje University, Gimhae 50834, Republic of Korea 

4: Department of Bio-Health Technology, Kangwon National University, Chuncheon 24341, Republic of Korea

 

摘要：Formation of an electrolyte complex using the electrostatic interactions between a polyanionic polymer and a cationic drug is a simple and efficient method of preparing a colloidal drug carrier system. Dextran sulfate, with a negatively charged sulfate group, was reacted in an acetate buffer solution of pH 3 with positively charged 1° amine, 2° amine, 3° amine, piperazine, and piperidine structures from 24 small-molecule drugs. The electrolyte complex was formed from 15 drugs, 63% of those tested. The tendency to form the electrolyte complex was in the order of piperazine and piperidine >3° amine >>2° amine. The drugs with the 1° amine structure failed to form an electrolyte complex. The mean particle sizes were in the range of 50-740 nm, and most of them showed a submicron colloidal dispersion of <400 nm. Regarding drug encapsulation efficiency (%), 11 drugs with piperazine, piperidine, and 3° amine structures showed 60–98% efficiency, which was fairly high. The results suggest that directly forming the electrolyte complex with dextran sulfate yields promising structural attributes as a submicron colloidal drug carrier system.

 

關鍵詞：Amine Structure; Dextran Sulfate; Electrolyte Complex; Submicron Drug Carrier System