DACLATASVIR DIHYDROCHLORIDE MICROSPHERES, PROCESS PARAMETERS FOR ENHANCED PERMEABILITY AND LIVER TARGETING

SUDHAMANI K; JEEVANA JYOTHI B

doi:10.22159/ajpcr.2022.v15i12.46596

Authors

SUDHAMANI K Depatment of pharmaceutics, Mallareddy Institute of Pharmaceutical Sciences, Affiliated to JNTUH, Hyderabad, Telangana, India. https://orcid.org/0000-0003-3117-6597
JEEVANA JYOTHI B Depatment of pharmaceutics, Sri Padmavati Mahila Visvavidyalayam, Tirupati, Andhra Pradesh, India.

DOI:

https://doi.org/10.22159/ajpcr.2022.v15i12.46596

Keywords:

Daclatasavir dihydrochloride, Emulsion crosslinking technique, Chitosan, Ex-vivo permeation studies

Abstract

Objectives: Daclatasavir dihydrochloride (DCLD) is used to treat hepatitis C. DCLD can be used to patients with all stages of compensated liver disease including cirrhosis. The aim of the present study was to develop DCLD microspheres to improve the permeation and maximum accumulation in the liver and in vitro evaluation.

Methods: DCLD microspheres were prepared with chitosan polymer using emulsion crosslinking technique. Twelve formulations were prepared, that is, F1-F12. The microspheres were evaluated for morphology, particle size, encapsulation efficiency, % yield, and permeability. FTIR studies were conducted on optimized formulation to check the drug-excipient compatibility.

Results: The particle size of microspheres was in the range of 11.50±0.08 μm to 98.50±0.05 μm. Encapsulation efficiency of the formulations was observed in the range 47.8–69.2%. The ex vivo permeation studies revealed that 83.3±0.1% of drug was diffused from microspheres in 60 min, whereas from pure drug 49±0.7% of drug was diffused in 60 min.

Conclusion: DCLD microspheres were shown good permeability when compared to pure drug which will improve the absorption.

Downloads

Download data is not yet available.

References

Rabaan AA, Al-Ahmed SH, Bazzi AM, Alfouzan WA, Alsuliman SA, Aldrazi FA, et al. Overview of hepatitis C infection, molecular biology, and new treatment. J Infect Public Health 2020;13:773-83.

Jagadabi V, Kumar PV, Mahesh K, Pamidi S, Ramaprasad LA, Nagaraju D. A stability-indicating UPLC method for the determination of potential impurities and its mass by a new QDA mass detector in daclatasvir drug used to treat hepatitis C infection. J Chromatogr Sci 2019;57:44-53.

Gamal N, Gitto S, Andreone P. Efficacy and safety of daclatasvir in hepatitis C: An overview. J Clin Transl Hepatol 2016;4:336-44.

Hassib ST, Taha EA, Elkady EF, Barakat GH. Reversed-phase liquid chromatographic method for determination of daclatasvir dihydrochloride and study of its degradation behavior. Chromatographia 2017;80:1101-7.

McCormack PL. Daclatasavir: A review of its use in adult patients with chronic hepatitis C virus infection drugs. Drugs 2015;75:515-24. doi: 10.1007/s40265-015-0362-5, PMID 25721433

He M, Wang H, Dou W, Chou G, Wei X, Wang Z. Preparation and drug release properties of norisoboldine-loaded chitosan microspheres. Int J Biol Macromol 2016;91:1101-9. doi: 10.1016/j.ijbiomac.2016.06.076

Dozie-Nwachukwu SO, Danyuo Y, Obayemi JD, Odusanya OS, Malatesta K, Soboyejo WO. Extraction and encapsulation of prodigiosin in chitosan microspheres for targeted drug delivery. Mater Sci Eng C Mater Biol Appl 2017;71:268-78.

Yan F, Li B, Shen F, Fu Q. Formulation and characterization of albumin microspheres containing norcantharidate for liver tumor targeting. Drug Deliv 2015;22:862-8. doi: 10.3109/10717544.2014.898715, PMID 24670098