Most of the biologically active constituents of plants or animals are polar or water soluble molecules. However, water soluble phytoconstituents such as vitamins,minerals,nutrients etc. are poorly absorbed either due to their large molecular size which cannot absorb by passive diffusion, or due to their poor lipid solubility; severely limiting their ability to pass across the lipid-rich biological membranes, resulting poor bioavailability.These types of drugs are then classified into biopharmaceutical classification system classes: high solubility/low permeability (Class III).
How to improve the bioavailaibility of these actives suggest suitable technique or delievery system?
You may try using liposome based drug delivery. As DNA transfection using lipofectamine.
Most of the lipid based vesicular delivery systems (liposomes, niosomes, bilosomes etc) were proven to be promising strategies in improving the systemic exposure of either solubility limited or permeability limited drugs. Even polymeric micelles was investigated to enhance the bioavailibility of challeneging molecules. However, the molecular weight of the molecule need tobe considered before one go for the startegy. Good number of research findings suggest that these systems was found to reliable in improving the bioavailibility of hydrophilic phytochemicals.
yes liposomes, niosomes etc can be used for enhancing bioavailability of drugs(class III). Also self emulsifying drug delivery systems play a major role in this aspect. First we should understand the factors responsible for the drugs poor bioavailability apart from solubility and permeability. I mean is the drug prone for gastric or .... degradation, drug metabolism, receptors that takepart in the absorption and distribution of drug, etc etc.
then we should design the DDS
You can work on niosomal drug delivery system as lot of research has been done for improving permeability of class III drugs via niosomal approch. Nonionic surfactants based vesicles have shown promising results for this issue.
Liposomes, nisosomes or transferosomes. Microemulsions and nanoemulsions maybe useful too
Hi Avinash,
if it is a real class III compound, the challenge is to increase permeability.
In this case, most common and reasonable approach is to make use of permeability enhancers, even if there is a payback for possible toxicity as well as unwanted absorption of other molecules present in the GI.
Use of ionic coupling to mask the polar portion of the molecule is another possible approach.
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