Hi everyone,
I am working on developing alginate/pectin beads in CaCl2 using ionic gelation method. The problem I am having is the low loading efficiency. I have tried all possible trials like, crosslinking time, the ratio of gel versus drug, the effect of concentration of gel/drug, the effect of alginate versus pectin ratio, etc but the maximum loading efficiency I am getting is 40 %. Any comments on how to increase the loading efficacy?
Cheers, H
The concentration of the polymers used to prepare the gel influences both the diffusion-based drug release kinetics and the degradation time of the hydrogel.
Dear all, 40% is not a low loading capacity, it almost close to the ultra-high loading of 50%. Anyway, generally to increase this value, one has to play on the affinity between drug/matrix by any interaction mechanism such as the one investigated in the following document. My Regards
https://doi.org/10.1021/jacs.7b12776
Dear Madhukar Baburao Deshmukh , Thank you for the comment. I have changed the ratio of gel versus drug and also prepared higher concentrations of the same ratio. For Alg:Pec:Drug 2.5g: 2.5g:3.4 g in 200 ml H2O, the loading efficiency was 12 mg by HPLC. So I increased the concentration of thw whole solution by keeping the ratio of gel:drug constant and I prepared Alg:Pec:Drug 5g: 5g:6.8 g in 200 ml H2O for which the loading drug was 8 mg. In the same 200 mL volume, I have more gel and API So I was expecting to get more loading but it is less? Any comments would be appreciated.
Dear Abdelkader BOUAZIZ thank you for the comment. I see in the literature reporting even 90 % loading efficacy but you consider 50 % ultra high? The second point is I am working in a pharma company and the excipients we use should not be toxic and also the set up for this covalent coordination is not available in our lab.
Dear Hossein Hetemadi, 90% of what ? Would you please give only on reference you have seen. My Regards
Dear Hossein Hetemadi, the following quote is taken from the reference I suggested. I think there is a confusion between two different parameters : loading capacity and loading efficiency.
'....micelles with ultrahigh drug loading (∼50%), nearly quantitative loading efficiency (>95%)....'
Dear Hossein Hetemadi, many thanks for posting this very interesting technical question on RG. I appreciate the answer of Abdelkader BOUAZIZ, do not confuse with % loading and loading efficiency. Loading efficiency is always greater than % loading.
Loading efficiency gives you an idea about the %drug that is successfully entrapped/adsorbed into nanoparticles. It is calculated as follows: %EE = [(Drug added - Free "unentrapped drug")/Drug added] *100 Example: If the %EE is 30%, it means that 30% of your drug is entrapped into the nanoparticles. Drug loading content helps you to deal with nanoparticles after their separation from the medium and to know their drug content. It is calculated using the following equation: Drug loading content (%)= (Weight of drug in nanoparticles/ Weight of nanoparticles)*100 Example: If the loading capacity is 30%, it means that 30% of the nanoparticle's weight is composed of the drug! i.e. Each 1 mg nanoparticles contains 0.3 mg drug.
There are also some relevant literature references available:
Article A functional chitosan-based hydrogel as a wound dressing and...
Good luck with your work!
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