Design and Evaluation of Efavirenz Loaded Solid Lipid Nanoparticle for Boosting Oral Bioavailability
DOI:
https://doi.org/10.37285/ijpsn.2021.14.6.8Abstract
Present work illustrates that efavirenz-loaded solid lipid nanoparticles were prepared with the objective of increasing bioavailability and protection of drugs due to biocompatible lipidic content. Efavirenz is generally used for the treatment of HIV. Selection of the suitable lipid phase, surfactant, and cosurfactant was done by individual screening method with the construction of pseudo-ternary phase study. The formulations were prepared by the microemulsion method followed by the lyophilization technique. EFV-SLN has shown a mean particle size of 55.73 ± 3.9 nm having a PDI of 0.153 ± 0.451. Zeta potential was found to be -9.98mV and the formulation was found stable. In vivo pharmaco-kinetic studies exhibited 5.41-fold enhancement in peak plasma concentration (
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Keywords:
Solid-lipid nanoparticles, Efavirenz, Pseudo-ternary phase study, Lipophilic, Bioavailability, Pharmacokinetics study
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Baert L, Schueller L, Tardy Y, Macbride D, Klooster GV, Borghys H, Clessens E, Mooter GVD, Gyseghem EV, Remoortere PV, Wigerinck P, and Rosier J (2008). Development of an implantable infusion pump for sustained anti-HIV drug administration. International Journal of Pharmaceutics 355 (1-2): 38–44.
Blasi P, Giovagnoli S, Schoubben A, Ricci M, and Rossi C (2007). Solid lipid nanoparticles for targeted brain drug delivery. Advanced Drug Delivery Reviews 59(6): 454–477.
Chiappetta DA, Hocht C, Taira C, and Sosnik A (2010). Efavirenz-loaded polymeric micelles for pediatric anti-HIV pharmaco-therapy with significantly higher oral bioavailability. Nanomedicine 5(1): 11–23.
Chime SA, Attama AA, Builders PF, and Onunkwo GC (2013). Sustained-release diclofenac potassium-loaded solid lipid microparticle based on solidified reverse micellar solution: in vitro and in vivo evaluation. Journal of Microencapsulation 30(4): 335–345.
Corbau R, Mori J, Phillips C, Fishburn L, Martin A, Mowbray C, Panton W, Smith-Burchnell C, Thornberry A, Ringrose H, Knochel T, Irving S, Westby M, Wood A, and Perros M (2010). Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. Antimicrobial Agents and Chemotherapy 54(10): 4451–4463.
Kalam MA, Sultana Y, Ali A, Aqil M, Mishra AK, and Chuttani K (2010). Preparation, characterization, and evaluation of gatifloxacin loaded solid lipid nanoparticles as colloidal ocular drug delivery system. Journal of Drug Targeting 18(3):191– 204.
Katara R and Majumdar DK (2013). Eudragit RL 100-based nanoparticulate system of aceclofenac for ocular delivery. Colloids and Surfaces B: Biointerfaces 103: 455–462.
Mehnert W and Mader K (2001). Solid lipid nanoparticles: production, characterization and applications. Advanced Drug Delivery Reviews 47(2-3): 165–196.
Mudgil M and Pawar PK (2014). Preparation and in Vitro/Ex Vivo evaluation of moxifloxacin loaded PLGA nanosuspensions for ophthalmic application. Scientia Pharmaceutica 81(2): 591–606.
Shafiq S, Shakeel F, Talegaonkar S, Ahmad FJ, Khar RK, and Ali A (2007). Design and development of oral oil in water ramipril nanoemulsion formulation: in vitro and in vivo evaluation. Journal of Biomedical Nanotechnology 3(1): 28-44.
Sood S, Jawahar N, Jain K, Kuppusamy G, and Meyyanathan S.N (2013). Olanzapine loaded cationic solid lipid nanoparticles for improved oral bioavailability. Current Nanoscience 9(1): 26–34.
Vatyam JM, Vani V, and Rao U (2014). Enhancement of solubility and dissolution rate of efavirenz using liquisolid compact technique. International Journal of Pharmacy 4(1): 150-156.
Wong HL, Wu XY, and Bendayan R (2012). Nanotechnological advances for the delivery of CNS therapeutics. Advanced Drug Delivery Reviews 64(7): 686–700.
