• K. Ramesh Jawaharlal Nehru Technological Institute Hyderabad, Hyderabad
  • Bonagiri ChandraShekar Bomma Institute of Pharmacy
  • Podile Khadgapathi Hetero Labs Ltd


Etravirine, Spray drying method, Soluplus, Povidone, Amorphous form


Objective: Current research work deals with the enhancement of solubility and dissolution of Poorly soluble Etravirine, which is belongs to BCS class-IV by Spray drying method (SD), which has been found to be the most widely used method in enhancing the solubility and rate of dissolution of poorly soluble drug substances.

Methods: Etravirine is belongs to BCS class-IV. It is insoluble in water and practically insoluble across the pH range of 1 - 6.8 of the major concerns with the Etravirine is its poor solubility, which results into poor bioavailability after oral administration. SD method has been proven to be an efficient method for conversion of poorly soluble crystalline polymorphic form into highly soluble amorphous form and make it useful for formulating lab scale batches to commercial batches. Hence, Spray drying method was chosen for converting poorly soluble crystalline form of Etravirine into highly soluble amorphous form using various carriers like Soluplus and Povidone (drug to polymer in 1:2 and 2:1 ratios) to increase its aqueous solubility and rate of drug release.

Results: There is almost 4 fold and 15 fold increases in the solubility of Etravirine prepared by SD as compared with Etravirine (crystalline form) in purified water and in pH 6.8 Phosphate buffer, respectively. From the characterization of spray dried powder of SD4 by Fourier Transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Powder X-ray diffraction (p-XRD), Scanning electron microscopy (SEM) concluded that crystalline Etravirine has been converted into an amorphous form. Faster and high drug release was found in the formulation of SD4.

Conclusion: The obtained results suggested that Spray drying method might be an efficacious approach for converting poorly soluble crystalline polymorphic form into highly soluble amorphous form and ultimately results in enhancing the therapeutic potential of Etravirine.



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Amit Chaudhary, Upendra Nagaich, Neha Gulati, VK Sharma, RL Khosa. Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: A recent review. J Adv Pharma Edu Res 2012;2(1):32-67.

TN Kakuda. Single and multiple–dose pharmacokinetics of Etravirine administered as two different formulations in HIV-1 infected patients. Antiviral Ther 2008;13:655–61.

Mohammed Jafar, Dehghan Mhg, Adil Shareef. Enhancement of Dissolution and anti-inflammatory effect of Meloxicam using solid dispersions. Int J Appl Pharm 2010;2(1):22-7.

Bhavesh B Patel, Jayvadan K Patel, Subhashis Chakraborty. Review: Revealing facts behind spray dried solid dispersion technology used for solubility enhancement. Saudi Pharm J 2014;1-14.

Yanbin Huang, Wei-Guo Dai. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharm Sin B 2014;4(1):18–25.

Advance of nano spray drying in pharmaceutical applications. Chinese J Pharm 2013;44(4):399-403.

Guy Van den Mooter. The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate. Drug Discov Today Technol 2012;9(2):79-85.

More Swati K, Wagh MP. Review on spray drying technology. Int J Pharm Chem Biological Sci 2014;4(2):219-25.

K Kolter, M Karl, A Gryczke. Hot-Melt extrusion with BASF polymers, Extrusion compendium2nd Revised and Compendium; 2012. p. 58-60.

Marieke Pudlas, Samuel O Kyeremateng, Leonardo AM Williams, James A Kimber, Holger van Lishaut, Sergei G Kazarian, et al. Analyzing the impact of different excipients on drug release behavior in hot-melt extrusion formulations using FTIR spectroscopic imaging. Eur J Pharm Sci 2015;67:21–31.

Ramesh K, Chandra Shekar Bonagiri, Khadgapathi Podile, DVRN Bhikshapathi. Formulation and evaluation of poorly soluble Etravirine by solid dispersions based hot-melt extrusion. An Int J Adv Pharm Sci 2014;5(6):2586–3000.

K Ramesh, B Chandra Shekar, P Khadgapathi, DVRN Bhikshapathi. Design and evaluation of tolvaptan solid dispersions using hot-melt extrusion and spray drying technique–A comparative study. Der Pharm Lett 2015;7(1):218-31.



How to Cite

Ramesh, K., B. ChandraShekar, and P. Khadgapathi. “FORMULATION AND EVALUATION OF POORLY SOLUBLE ETRAVIRINE BY SPRAY DRYING METHOD”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 4, Apr. 2015, pp. 98-103,



Original Article(s)