Formulation and Evaluation of Lipid Based Nanoparticles of Etravirine

  • Tripura Sundari I Bala Department of Pharmaceutics, Sri Venkateshwara College of Pharmacy, Madhapur, Hyderabad, India
  • C.V.S Subramanyam HOD, Department of Pharmaceutics Gokaraju Rangaraju College of Pharmacy, Hyderabad, India


Engineered nanoparticles have the potential to revolutionize the diagnosis and treatment of many diseases like HIV/AIDS. Etravirine is one of the key components of highly active antiretroviral therapy used for the treatment of HIV-1 infections. The aim of the present study was to formulate and evaluate nanostructured lipid carriers of etravirine, intended for targeted delivery to macrophages, using solvent emulsification - evaporation technique.  Estimates of drug solubility were employed for selection of solid lipids, liquid lipids and stabilizers for the preparation of NLCs. Design of experiments was used to optimize the formulation with respect to drug-lipid ratio and concentration of stabilizer in the external phase using 32 full factorial design. Particle size of the carriers and drug release characteristics were the responses which were set to suitable levels for optimization. The optimized formulation was prepared and characterized for size, poly dispersity index, zeta potential, entrapment efficiency and appearance. The nanostructured lipid carriers of etravirine were prepared using stearylamine and glyceryl monostearate as solid lipids, Capryol 90 as liquid lipid and polyvinyl pyrrolidone as stabilizer. All experimental batches showed high drug loading efficiencies nearing 99%, indicating that etravirine remained closely associated with the lipids. The nanostructured lipid carriers displayed a zeta potential of -10.1 mv and a particle size of 261.6 nm with a polydispersity index of 0.374. In vitro release of etravirine from the optimized formulation at 2 h was 9% indicative of a low burst; and 56% of the entrapped drug was released after 24 h, suggesting prolonged release characteristics. Thus, etravirine loaded lipidic nanoparticles with potential for targeting cellular reservoirs of the AIDS virus such as macrophages were successfully developed.

Keywords: Etravirine, Nanostructured lipid carriers, full factorial design

Keywords: Etravirine, Nanostructured lipid carriers, Full factorial design


Download data is not yet available.

Author Biographies

Tripura Sundari I Bala, Department of Pharmaceutics, Sri Venkateshwara College of Pharmacy, Madhapur, Hyderabad, India

Department of Pharmaceutics, Sri Venkateshwara College of Pharmacy, Madhapur, Hyderabad, India

C.V.S Subramanyam, HOD, Department of Pharmaceutics Gokaraju Rangaraju College of Pharmacy, Hyderabad, India

HOD, Department of Pharmaceutics Gokaraju Rangaraju College of Pharmacy, Hyderabad, India


1. Kongnyuy EJ, Soskolne V, Adler B, "Hormonal contraception, sexual behaviour and HIV prevalence among women in Cameroon" BMC Women's health, 2008; 8(1):1-6. PMid:18973697 PMCid:PMC2584627
2. Freed E.O, Englund. G, Martin M.A, "Role of the basic domain of human immunodeficiency virus type 1 matrix in macrophage infection" Journal of virology, 1995; 69(6):3949-3954. PMid:7745752 PMCid:PMC189124
3. Goff SP, "Genetics of retroviral integration" Annual review of genetics, 1992; 26(1):527-544. PMid:1482125
4. Narayan O, Clements JE, "Biology and pathogenesis of lentiviruses" Journal of General virology, 1989; 70(7):1617-1639. PMid:2544657
5. Rajnish S. Dave, Pooja Jain, Siddappa N. Byrareddy, "Follicular dendritic cells of lymph nodes as human immunodeficiency virus reservoirs and insights on cervical lymph node" Front. Immunol, 2018; 9: 1-8. PMid:29725333 PMCid:PMC5916958
6. Alexaki A, Liu Y, Wigdahl B, "Cellular reservoirs of HIV-1 and their role in viral persistence" Current HIV research, 2008; 6(5):388-400. PMid:18855649 PMCid:PMC2683678
7. Das Neves J, Amiji MM, Bahia MF, Sarmento B, "Nanotechnology-based systems for the treatment and prevention of HIV/AIDS" Adv. Drug Deliv. Rev, 2010; 62(4):458-477. PMid:19914314
8. Bonyhadi ML, Rabin L. Salimi S, Brown D A, Kosck J, Mc Cune JM, Kaneshima H, "HIV induces thymus depletion in vivo" Nature 1993; 363 (6431):728-732. PMid:8100043
9. Gunaseelan S, Gunaseelan K, Deshmukh M, Zhang X, Sinko PJ, "Surface modification of nanocarriers for effective intracellular delivery of anti-HIV drugs" Advanced drug delivery reviews 2010; 62(4):518-531. PMid:19941919 PMCid:PMC2841563
10. Adema GJ, Hartgers F, Verstraten R, Vries E de, Marland G, Menon S, Foster J, Xu Y, Nooyen P, McClanahan T, "A dendritic-cell derived CC chemokine that preferentially attracts naive cells" Nature Journal 1997;387(6634):713-720. PMid:9192897
11. Vasir JK Reddy MK, Labhasetwar VD, "Nano systems in drug targeting Opportunities and challenges" Current Nanoscience 2005; 1(1): 47-64.
12. Mallipeddi R, Rohan LC, "Progress in antiretroviral drug delivery using nanotechnology" International journal of nanomedicine 2010; 5(1):533-547. PMid:20957115 PMCid:PMC2950411
13. Chauhan I, Yasir M, Verma M, Singh AP, "Nanostructured Lipid Carriers: A Groundbreaking Approach for Transdermal Drug Delivery" Adv Pharm Bull. 2020;10 (2):150-165. PMid:32373485 PMCid:PMC7191226
14. Johnson LB, Saravolatz LD, "Etravirine, a next generation non-nucleoside reverse transcriptase inhibitor" Clin infect Dis 2009; 48:1123-1128. PMid:19275497
15. Adams J, Patel N, Mankaryous N, Tadros M, Miller CD, "Non-nucleoside reverse transcriptase inhibitor resistance and the role of the second-generation agents" Ann Pharmacother 2010; 44:157-165. PMid:19996323
16. Scholler Gyure M, Kakuda TN, Raoof A, De Smedt G, Hoetelmans RM, "Clinical pharmacokinetics and pharmacodynamics of etravirine" Clin Pharmacokinetics 2009; 48:561-574. PMid:19725591
17. Chakravarthy, M, Vora, A, "Nanotechnology based anti-viral therapeutics" Drug Delivery and Transl Res 2021; 11(3):748-787. PMid:32748035 PMCid:PMC7398286
18. Chen, Y, Yang, X, Zhao, L, Almasy, L, Garamus, V.M, Willumeit, R, Zou, "A Preparation and Characterization of nano structured lipid carrier for a poorly soluble drug" Colloids surfaces A Physicochem. Eng. ASP 2014; 455(1):36-43.
19. Jindal, A.B, Bachhav, S.S, Devarajan, P.V "In-situ hybrid nano drug delivery system of anti-retroviral drug for simultaneous targeting to multiple viral reservoirs: an in vivo proof of concept" Int J. Pharm.2017; 521(1):196-203. PMid:28229943
20. Nagaich, U, Gulati, N, "Nanostructured lipid carriers (NLC) based controlled release topical gel of Clobetasol propionate: design and in vivo characterization" Drug delivery. Transl Res 2016; 6(1):289-298. PMid:27072979
21. Shete, H, Patravale, V "Long chain lipid-based tamoxifen NLC. Part 1: Preformulation studies, formulation development and physicochemical characterization" Int. J.Pharm. 2013; 454(1):573-583. PMid:23535345
22. Soni, M, Shelkar, N, Gaikwad, R, Vanage, G, Samad, A, Devarajan, P. "Buparvaquone loaded solid lipid Nanoparticles for targeted delivery in theleriosis", J.Pharm. Bioallied Sci. 2014; 6(1):22-30. PMid:24459400 PMCid:PMC3895290
23. G.B. Preethi, H.N. Shivakumar, M. Ravi Kumar. N. Swetha. "Prototype self-emulsifying system of Etravirine: design, formulation and in vitro evaluation" Int. J. App. Pharm 2018;10 (2):13-19.
24. Wissing SA, Muller RH, Radtke M. "Nanostructured lipid matrices for improved microencapsulation of drugs" Int J Pharm 2002; 242(1):121-128. PMid:12176234
25. Elmowafy M, Al-Sanea MM "Nanostructured lipid carriers (NLCs) as drug delivery platform: Advances in formulation and delivery strategies" Saudi Pharm J 2021; 29(9): 999-1012. PMid:34588846 PMCid:PMC8463508
26. Sarvesh Bohrey, Vibha Chourasiya, Archna Pandey "Polymeric nanoparticles containing diazepam: preparation, optimization, characterization, in-vitro drug release and release kinetic study" Nano convergence 2016; 3(3):1-7. PMid:28191413 PMCid:PMC5271152
27. Chauhan I, Yasir M, Verma M, "Nanostructured Lipid Carriers: A Groundbreaking Approach for Transdermal Drug Delivery" Adv Pharm Bull 2020;10(2):150-165. PMid:32373485 PMCid:PMC7191226
28. Satish Rojekar, Leila Fotooh Abadi, Rohan Pai, Ketan Mahajan, Smita Kulkarni, Pradeep R Vavia "multi organ targeting of HIV-1 viral reservoirs with etravirine loaded nanostructured lipid carrier: An In vivo proof of concept" Eur. J. Pharm. Sci 2021;164:1-18. PMid:34166780
29. Yang Wang, Wei Wu "in situ evading of phagocytic uptake of stealth nanoparticles by mouse peritoneal macrophages" Drug Delivery 2006;13(1):189-192. PMid:16556570
30. Raveen Parboosing. Glenn E. M. Maguire, Patrick Govender, Hendrik G. Kruger "Nanotechnology and the treatment of HIV infection", viruses MDPI 2012; 4(4):488-520. PMid:22590683 PMCid:PMC3347320
31. G. U. Sailor, V. D. Ramani, N. Shah, G. R. Parmar, Dipti Gohil, R. Balaramani, A. Sethi "Design of experiment approach-based formulation optimization of Berberine loaded solid lipid nanoparticle for antihypertensive activity" Indian J. Pharm. Sci. 2021; 83(2):204-218.
32. Almousallam, M, Moia C, Zhu H "Development of nanostructured lipid carrier for dacarbazine delivery" Int Nano Lett 2015; 5:242-248.
33. Song, S.H. Lee, K.M, Kang, J. B. Lee, S.G. Kang, MJ, Choi, Y.W "improved skin delivery of voriconazole with a nanostructured lipid carrier-based hydrogel formulation" Chem. Pharm. Bull 2014; 62(8):793-798. PMid:25087631
34. Siahdasht FN, Farhadian N, Karimi M. Hafizi. L "Enhanced delivery of melatonin loaded nanostructured lipid carriers during in vitro fertilization: NLC formulation, optimization and IVF efficacy" RSC ADV 2020; 10(16):9462-9475. PMid:35497203 PMCid:PMC9050139
35. Fang Cl, Suwayeh AS, Fang JY "Nanostructured lipid carriers (NLCs) for drug delivery and targeting" Recent Pat Nanotechnology 2013; 7(1):41-55. PMid:22946628
36. Fotooh Abadi, L; Damiri, F; Zehravi, M; Joshi, R; Pai, R; Berrada, M; Massoud, E. E. S; Rahman, M. H; Rojekar, S; Cavalu, S. Novel Nanotechnology-based approaches for targeting HIV Reservoirs" Polymers 2022;14(15):1-26. PMid:35956604 PMCid:PMC9370744
91 Views | 19 Downloads
How to Cite
Bala TSI, Subramanyam C. Formulation and Evaluation of Lipid Based Nanoparticles of Etravirine. JDDT [Internet]. 15Jan.2024 [cited 25Feb.2024];14(1):79-0. Available from: