Novel Biopolymeric Microspheres for Colon-Targeted Peptide Drug Delivery: An in vitro Investigation

Background

Vancomycin (VAN) is used as a model peptide. It has been used extensively to treat severe infections brought on by Gram-positive bacteria. Vancomycin in colon-targeting studies has its therapeutic relevance in treating colonic infections, particularly antibiotic-associated colitis caused by Clostridioides difficile. The use of polymers like Eudragit S100 enables pH-dependent release, protecting the drug in the small intestine and stomach while promoting release in the area of the colon. Similarly, biodegradable carriers such as Gelatin can enhance encapsulation and controlled drug release.

Purpose

Because of the drugs physicochemical characteristics, poor upper GI absorption, peptide-like behavior, and clinical relevance in colonic diseases, vancomycin is a great model medication while developing and testing colon-targeted drug delivery systems. An oral formulation with sustain release targeted to the colon would serve as an ideal formulation.

Materials and Method

The emulsification method was used to develop microparticles. VAN was enteric coated with Eudragit S-100 after being trapped in a gelatine microsphere. The morphology, particle size, encapsulation effectiveness, and drug release of the microspheres were all evaluated.

Result and Conclusion

According to the initial research, gelatine and Eudragit S-100 were compatible with VAN. The peptide can be trapped by these microspheres at high concentrations, where the drug's inner gelatin core would enable kinetic control of release and coating guarantees the digestive tract's medication core localisation. For the oral administration of peptide medications like vancomycin, enteric coated cross-linked gelatin microspheres show promising potential.