Preparation and Characterization of Berberine-loaded Dextrose-modified Nanostructured Lipid Carriers

Author: Neelu Singh, Himanshu Bhaskar and Shubhini A. Saraf

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Abstract

Rheumatoid arthritis (RA) is an autoimmune ailment that manifests rapidly in troublesome locomotive activity and often restricted movements in patients. The conventional therapy for RA is done through NSAIDs but often showed unsatisfactory therapeutic outcomes. Recently nature derived anti-arthritic phytoconstituents have been explored for RA therapy. Berberine (Br) has attained considerable attention as a natural xenobiotic for RA therapy. However, its use is restricted due to extensive first-pass elimination, low aqueous solubility, low permeability, and low oral bioavailability. Lipodal drug delivery systems can address these challenges thus in the present research, we have formulated dextrose (DEX) modified Br-loaded Nanostructured Lipid Carriers (NLCs) employing the melt-emulsification method. The prepared DEX-Br-NLCs were assessed for percent entrapment, drug loading, in-vitro release and cytotoxicity on HEK-293T cells. The prepared DEX-Br-NLCs exhibited a particle size of 200.9±0.53 nm, percent entrapment of 68.42±1.51%, drug loading of 3.58±0.14% and 80.32±6.65% drug release respectively over a period of 24 hr. Internalization of Rhodamine loaded DEX-Br- NLCs was confirmed via cellular uptake study. Cytotoxicity studies revealed that the prepared formulation was non-toxic. Thus DEX-Br-NLCs were successfully prepared, which might further improve the oral bioavailability, solubility and permeability of Br and produced controlled release of the drug localized inflammation.

Keywords

Berberine, Rheumatoid arthritis, NLCs, Complete Freund’s adjuvant, Auto-immune

Conclusion

In summary, DEX-Br-NLCs were prepared successfully. Results indicate that the entrapment of Br into NLCs showed great potential to deliver the drug efficiently to the predetermined desired site witnessing shielding effect on the encased drug during transit against the wide pH variability throughout GIT, HEK293T cells showed no significant toxicity. The in vitro release studies displayed that the formulated lipid matrix delivered a controlled release drug and the stability studies demonstrated that NLCs were stable when stored for a long period.

References

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How to cite this article

Neelu Singh, Himanshu Bhaskar and Shubhini A. Saraf (2023). Preparation and Characterization of Berberine-loaded Dextrose-modified Nanostructured Lipid Carriers. Biological Forum – An International Journal, 15(5): 974-980.