The weakly acidic drugs icaritin (Scheme 1A), diosmin (Scheme 1B) and ibuprofen (Scheme 1C) were encapsulated in polymeric micelles by the ABS method. In brief, the weakly acidic drug (2.40 g for icaritin, 1.20 g for diosmin and ibuprofen) was dissolved in 0.2 mol/L sodium hydroxide aqueous solution (120 mL) to obtain the base solution of the drug. Soluplus® (9.6 g) and P407 (4.8 g) were dissolved in 0.05 mol/L hydrochloric acid aqueous solution (480 mL) to acquire the acid solution with the polymers. Then the base solution was added into the acid solution dropwise under magnetic stirring (1000 rpm) followed by centrifugation for 20 min at 10,000 rpm to gain the weakly acidic drug-loaded polymeric micelles solution. The ultrafiltration (polyethersulfone membrane, 100 KD) could be used to concentrate the resultant polymeric micelles solution.

Remdesivir (Scheme 1D) was selected to be the representative weakly alkaline drug. Remdesivir-loaded polymeric micelles were prepared via the ABS method. In short, remdesivir (1.11 g), Soluplus® (4.0 g), P407 (2.0 g) and concentrated hydrochloric acid (1.7 mL) were all dissolved in purified water (100 mL). A certain volume of the sodium hydroxide aqueous solution (8.0 mol/L) was then added into the resultant acid solution dropwise under magnetic stirring (1000 rpm) to adjust the pH of the solution to be 5.0. The Remdesivir-loaded polymeric micelles solution was obtained following centrifugation for 20 min at 10,000 rpm.

Icaritin (160 g) was dissolved in 0.2 mol/L sodium hydroxide aqueous solution (8 L) to obtain the base solution of the drug. Soluplus® (640 g), P407 (320 g) and 0.05 mol/L hydrochloric acid aqueous solution (32 L) were added to a glass reactor (50 L) and stirred (1000 rpm) for 2 h. Then, the base solution was pumped into the acid solution over 30 min under stirring (1000 rpm) at 20 °C. IPMs were obtained by centrifugation for 20 min at 10,000 rpm.

Fluorophore-labelled Icaritin−Cy5 and Icaritin−Cy5.5 were synthesized (Figure S1), and FRET micelles were prepared by ethanol the injection-dialysis method. Briefly, Icaritin−Cy5 (0.5 mg), Icaritin−Cy5.5 (0.5 mg) and icaritin (9.0 mg) were dissolved in ethanol (1 mL) to obtained the drug solution, and Soluplus® (40 mg) and P407 (20 mg) were dissolved in deionized water (8 mL) to gain the aqueous phase. The drug solution was then injected into the above aqueous phase under stirring at 1000 rpm. The FRET micelles were finally obtained by dialysis (MWCO: 3500 Da) against deionized water for 48 h to remove residual ethanol.

Note: The content above has been extracted from a research article, so it may not display correctly.



Q&A
Please log in to submit your questions online.
Your question will be posted on the Bio-101 website. We will send your questions to the authors of this protocol and Bio-protocol community members who are experienced with this method. you will be informed using the email address associated with your Bio-protocol account.



We use cookies on this site to enhance your user experience. By using our website, you are agreeing to allow the storage of cookies on your computer.