Characterization of Solid Binary Systems of Efavirenz and Hydroxypropyl-β-Cyclodextrin

Authors

  • Bharati Arali Department of Pharmaceutics, East West College of Pharmacy, Bengaluru, India
  • Anand Kumar Y Department of Pharmaceutics, V.L. College of Pharmacy , Raichur, India
  • Mallikarjuna Setty C Department of Pharmaceutics, Oxford College of Pharmacy, Bengaluru, India

DOI:

https://doi.org/10.21276/IJRDPL.2278-0238.2019.8(1).15-20

Keywords:

Efavirenz, Hydroxypropyl-?-cyclodextrin, solid binary systems, Solubility, Dissolution

Abstract

Efavirenz is a widely prescribed anti-retroviral drug that belongs to BCS class II and exhibit low and variable oral bioavailability due to its poor aqueous solubility and it requires enhancement in solubility and dissolution rate for increasing its oral bioavailability. The aim of this study was to increase the solubility of Efavirenz (EFA) by complexing it with Hydroxypropyl-β-cyclodextrin (HPβCD). Solid binary systems were prepared by co-grinding and microwave irradiation methods. The interaction of EFA with HPβCD was evaluated by Phase solubility studies, in vitro dissolution studies and different analytical techniques including Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). The apparent stability constant revealed EFA with HPβCD produces 1:1 M stoichiometric complex. The host guest interactions studied by FTIR and DSC confirmed true inclusion of EFA with HPβCD at 1:2 M. The Dissolution rates of EFA- HPβCD binary systems were faster when compared to physical mixture and pure drug. Overall the rank order of improvement in dissolution properties of Efavirenz with ratios is 1:2M > 1:1M and methods MW > CG > PM > Pure drug. One-way ANOVA suggest the DP60 and DE60 values were significantly higher (P<0.05) in solid binary systems prepared by microwave irradiation method when compared to co-grinding and its corresponding physical mixtures and pure drug.

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References

Maurin MB, Rowe SM, Blom K and Pierce ME. Kinetics and mechanism of hydrolysis of efavirenz. Pharm Res.2002; 19(4):517-522.

Chiappetta DA, Hocht C and Sosnik A. A highly concentrated and taste-improved aqueous formulation of efavirenz for a more appropriate pediatric management of the anti-HIV therapy. Curr HIV Res. 2002; 8(3):223-231.

Gazzard B, Bernard AJ, Bof?to M, Churchill D, Edwards S, Fisher N, Geretti AM, Johnson M, Leen C, Peters B, Pozniak A, Ross J, Walsh J, Wilkins E and Youle M. British HIV Association (BHIVA) guidelines for the treatment of HIV-infected adults with antiretroviral therapy. HIV Med. 2006; 7(8):487-503.

Kasim NA, Whitehouse M, Ramachandran C, Bermejo M, Lennernas H, Hussain AS, Junginger HE, Stavchansky SA, Midha KK, Shah VP and Amidon GL. Molecular properties of WHO essential drugs and provisional biopharmaceutical classi?cation. Mol Pharm. 2004; 1(1):85-96.

Takano R, Sugano K, Higashida A, Hayashi Y, Machida M, Aso Y and Yamashita S. Oral absorption of poorly water-soluble drugs: Computer simulation of fraction absorbed in humans from a mini scale dissolution test. Pharm Res. 2006; 23(6): 1144-1156.

Sosnik A, Chiappetta DA and Carcaboso AM. Drug delivery systems in HIV pharmacotherapy: What has been done and the challenges standing ahead. J Control Release. 2009; 138(1): 2-15.

Vasconcelos T, Sarmento B and Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water-soluble drugs. Drug Discov Today. 2007; 12(23-24): 1068-1075.

Kaplan S. Biopharmaceutical considerations in drug formulation design and evaluation. Drug Metab Rev. 1972; 1: 15-34.

Sathigari S, Chadha G, Lee YH, Wright N, Parsons DL, Rangari VK, Fasina O and Babu RJ. Physicochemical characterization of efavirenz-cyclodextrin inclusion complexes. AAPS PharmSciTech. 2009; 10(1): 81-87.

Dais ME and Brewster ME. Cyclodextrin based pharmaceutics: past, present and future. Nat Rev Drug Discov. 2004; 1023- 1035.

Viega F, Pecorelli C, and Ribeiro L. As Ciclodextrinas em Tecnologia Farmaceutics. Minerva Coimbra. 2006; 12- 78.

Challa R, Ahuja A, Ali J and Khar RK. Cyclodextrins in drug delivery: an updated review. AAPS Pharm Sci Tech. 2005; 6: 329-357.

Yap KL, Liu X, Thenmozhiyal JC and Ho PC. Eur J Pharm. Sci. 2005; 25: 49-56.

R G Strickley. Pharm Res. 2004; 21(2): 201-227.

Higuchi T and Connors KA. Advances in analytical chemistry and instrumentation. Wiley-interscience, New York. 1965; 4: 117-212.

Rumondor AC, Marsac PJ, Stanford LA and Taylor LS. Phase behavior of poly vinyl pyrrolidone containing amorphous solid dispersions in the presence of moisture. MolPharm. 2009; 6(5): 1492-1505.

Shown I. Banerjee S, Ramchandran AV and Geckeler KE, Murthy CN. Synthesis of Cyclodextrin and Sugar-Based Oligomers for the Efavirenz Drug Delivery. Macromol Symp. 2010; 287: 51-59.

Madhavi BB, Kusum B, Krishna Chatanya CH, Madhu MN, Sri Harsha V and Banji D. Dissolution enhancement of efavirenz by solid dispersion and PEGylation techniques. Int J Pharm Investig. 2011; 1: 29-34.

How to cite this article:

Bharati A, Kumar AY and Setty MC. Characterization of Solid Binary Systems of Efavirenz and Hydroxypropyl-β-Cyclodextrin. Int. J. Res. Dev. Pharm. L. Sci. 2019; 8(1): 15-20. doi: 10.13040/IJRDPL.2278-0238.8(1).15-20

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Published

2019-01-15

How to Cite

Arali, B. ., Kumar Y, A. ., & Setty C, M. (2019). Characterization of Solid Binary Systems of Efavirenz and Hydroxypropyl-β-Cyclodextrin. International Journal of Research and Development in Pharmacy & Life Sciences, 8(1), 15-20. https://doi.org/10.21276/IJRDPL.2278-0238.2019.8(1).15-20

Issue

Vol. 8 No. 1 (2019): Volume 8 Issue 1, January - February (2019)

Section

Original Article
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This work is licensed under a Creative Commons Attribution-NoDerivatives 4.0 International License.