Abstract
Background: Nature has always been considered as the primary source of pharmaceutical ingredients. A variety of hemicelluloses, as well as their modified forms, have been under investigation. Herein, a study was designed to explore the biocompatibility of hemicellulose and its modified form (thiolated hemicellulose) as well as its potential as a pharmaceutical excipient. Method: For thiol modification thiourea was used as the thiol donor, HCl as the catalytic reagent, and methanol was used for washing purposes. Modified polymers were characterized for physicochemical characteristics, including surface morphology, the amorphous or crystalline nature of the particles, modification of polymer by FTIR, and biocompatibilities. For acute oral toxicity study, a single dose of 2 g/kg was administered to albino rats of 200 g average weight (n = 3). Polymers were evaluated as pharmaceutical excipients by preparing compressed tablets of antiplatelet drug (Ticagrelor), followed by various quality control tests, such as swelling index, thickness and diameter, disintegration, and in-vitro drug release. Results: From the results, it was observed that thiol modification has been successfully accomplished as characteristic peaks belonging to –SH group appeared at 2667.7691 cm−1 in FTIR scan. The modified polymer was found safe in the use concentration range, confirming their safe use for in vivo analysis. No significant effect has been observed in the behavior, biological fluid (blood), or on vital organs. Thiolated hemicellulose was found to be an excellent drug retarding polymer as 8 h of dissolution studies showed that 67.08% of the drug has been released. Conclusion: Conclusively, incorporation of thiol moiety made the polymer more mucoadhesive with, and a worthy carrier of, the drug with good biocompatibilities.
Highlights
Research into the field of drug discovery and drug development by professional teams of pharmacists, scientists, clinicians, and statisticians is being done to contribute toward the betterment of human care
From the results, it was observed that thiol modification has been successfully accomplished as characteristic peaks belonging to –SH group appeared at 2667.7691 cm−1 in FTIR scan
Hemicellulose is mainly used as a mucoadhesive polymer and the strength of mucoadhesion is enhanced by modifying the structure via attaching a thiol moiety in the polymeric backbone (Zaman et al, 2018a)
Summary
Research into the field of drug discovery and drug development by professional teams of pharmacists, scientists, clinicians, and statisticians is being done to contribute toward the betterment of human care. Research into new drug deliveries has widely used polymers as an integral part in the development and advancement of medicine They are being fabricated in hydrogels, microspheres, nanoparticles, and modified release tablets, providing controlled and targeted drug delivery, enhancing the efficacy. Many efforts are being made to increase the absorption of less soluble and less permeable drugs through mucosal membranes Some of these efforts involve the conjugation of a drug with a thiomer, which greatly improves the mucoadhesive properties following enhanced bioavailability. Thiol modification of natural polysaccharides such as chitosan, alginate, pectin, and tamarind seed xyloglucan has been successfully done to improve their functional properties In pharmaceutical applications these modified polymers are effectively working as drug carriers (Bhatia and Ahuja, 2013). A study was designed to explore the biocompatibility of hemicellulose and its modified form (thiolated hemicellulose) as well as its potential as a pharmaceutical excipient
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