I can not have more than 13% of nanoencapsulation efficiency for two drugs of different properties (Specifications below).
What should be done in order to increase this efficiency of encapsulation? Which are the critical parameters that I should concern the more?
I’m synthetizing nanospheres by the emulsion/solvent evaporation technique. The devised nanosphere may encapsulate: One hydrophobic drug (pKa values of 1,7 and 7,9) and one hydrophilic drug (pKa values of 3,35 and 13,61).
Thanks in advance!
I think you are using a hydrophobic polymer. In this case, you can add hydrophobic drug with hydrophobic polymers by dissolving in suitable organic solvent. Encapsulation of hydrophilic drug may be difficult unless you use add a polymer with dual character or add a hydrophilic polymer. The best way will be to prepare core shell microspheres, one part of which will be hydrophilic and other hydrophobic. You can also go for liposomes that are usually preferred for the drugs of different philicities..
In addition to Rehman's suggestions, you can also make trial with changing core: coat ratios, and preparation parameters ( change of solvents, variation of rotation or agitation etc.,), you may get good drug encapsulation.
My suggestion would be to have a comparative check on different hydrophobic polymer. Different polymers will give you different EE. Also, drug to polymer ratio plays an important role.
Secondly, change of solvents, stirring rate also affect the encapsulation efficiency.
Also look into the type of stirrer you are using. Sharp blades may inc the chances of breaking of matrix.
Good Luck
I assume you are using hydrophobic polymer like PLGA. There should be no problem with the hydrophobic drug, just add it to the oil phase and you will get high EE.
For the hydrophilic drug, make the preparation method to be double-emulsion, the internal aqueous phase: change the pH to make the drug non-ionized, same goes to the outer aqueous phase. This will change the solubility of the drug to become less soluble in the buffer and hence higher EE is expected.
Other approaches to enhance EE: apply some vacuum to fasten the hardening step, add co-solvent that mix with water like acetonitril or ethyl acetate to fasten the hardening.
If both drugs can dissolve in the oil phase by using solvent mixture: like one in DCM and the other in methanol then mix.. this will be the best.
Good luck
Thanks so much for your time and valuable feedback! For sure, the experiment will be accomplished.
Hope I can have new and better results soon!
Best regards,
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