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Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate.
Mater Sci Eng C Mater Biol Appl. 2017 Sep 01; 78:1023-1034.MS

Abstract

Poor aqueous solubility of drugs has emerged as a major issue for pharmaceutical scientists from many decades. The current study explores the manufacture and development of a thermodynamically stabilized solid crystal suspension (SCS) of poorly water soluble drug efavirenz via hot melt extrusion. Efavirenz is a non-nucleoside reverse transcriptase inhibitor and belongs to BCS class II. The SCS was prepared using pearlitol and xylitol as a crystalline carrier. The drug-excipient blend was processed by hot melt extrusion with up to 50% (w/w) drug loading. Physico-chemical characterization of the SCS conducted via a scanning electron microscopy, differential scanning calorimetry and hot stage microscopy confirmed that SCS are in crystalline state. Similarly, X-ray powder diffraction analysis revealed highly crystalline existence of pure drug, crystalline carriers and developed SCS. The FTIR chemical imaging analysis of SCS formulations showed a homogeneous drug distribution within respective crystalline carriers while an advanced chemical analysis via atomic force microscopy and Raman analysis complemented the foregoing findings. The developed SCS1 formulation showed up to 81 fold increase in the solubility and 4.1 fold increase in the dissolution rate of the drug compared to that of the bulk substance. Surprisingly, the developed SCS formulation remained stable for a period of more than one year at accelerated conditions inferred from dissolution studies. It can be concluded that the SCS approach can be used as an alternative contemporary technique to enhance the dissolution rates of many other poorly water-soluble drugs by means of thermal HME processing.

Authors+Show Affiliations

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400019, Maharashtra, India. Electronic address: ph13jn.pawar@pg.ictmumbai.edu.in.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400019, Maharashtra, India; Faculty of Pharmaceutics Department, H.K. College of Pharmacy, Relief Road, Oshiwara, Jogeshwari West, Mumbai 400102, Maharashtra, India.Department of Pharmacy (Chemistry), School of Life Sciences, University of Sussex, Falmer, Brighton BN1 9QT, United Kingdom. Electronic address: M.Maniruzzaman@sussex.ac.uk.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400019, Maharashtra, India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28575936

Citation

Pawar, Jaywant N., et al. "Solid Crystal Suspension of Efavirenz Using Hot Melt Extrusion: Exploring the Role of Crystalline Polyols in Improving Solubility and Dissolution Rate." Materials Science & Engineering. C, Materials for Biological Applications, vol. 78, 2017, pp. 1023-1034.
Pawar JN, Fule RA, Maniruzzaman M, et al. Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate. Mater Sci Eng C Mater Biol Appl. 2017;78:1023-1034.
Pawar, J. N., Fule, R. A., Maniruzzaman, M., & Amin, P. D. (2017). Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate. Materials Science & Engineering. C, Materials for Biological Applications, 78, 1023-1034. https://doi.org/10.1016/j.msec.2017.04.055
Pawar JN, et al. Solid Crystal Suspension of Efavirenz Using Hot Melt Extrusion: Exploring the Role of Crystalline Polyols in Improving Solubility and Dissolution Rate. Mater Sci Eng C Mater Biol Appl. 2017 Sep 1;78:1023-1034. PubMed PMID: 28575936.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate. AU - Pawar,Jaywant N, AU - Fule,Ritesh A, AU - Maniruzzaman,Mohammed, AU - Amin,Purnima D, Y1 - 2017/04/28/ PY - 2016/12/14/received PY - 2017/04/10/accepted PY - 2017/6/4/entrez PY - 2017/6/4/pubmed PY - 2018/3/15/medline SP - 1023 EP - 1034 JF - Materials science & engineering. C, Materials for biological applications JO - Mater Sci Eng C Mater Biol Appl VL - 78 N2 - Poor aqueous solubility of drugs has emerged as a major issue for pharmaceutical scientists from many decades. The current study explores the manufacture and development of a thermodynamically stabilized solid crystal suspension (SCS) of poorly water soluble drug efavirenz via hot melt extrusion. Efavirenz is a non-nucleoside reverse transcriptase inhibitor and belongs to BCS class II. The SCS was prepared using pearlitol and xylitol as a crystalline carrier. The drug-excipient blend was processed by hot melt extrusion with up to 50% (w/w) drug loading. Physico-chemical characterization of the SCS conducted via a scanning electron microscopy, differential scanning calorimetry and hot stage microscopy confirmed that SCS are in crystalline state. Similarly, X-ray powder diffraction analysis revealed highly crystalline existence of pure drug, crystalline carriers and developed SCS. The FTIR chemical imaging analysis of SCS formulations showed a homogeneous drug distribution within respective crystalline carriers while an advanced chemical analysis via atomic force microscopy and Raman analysis complemented the foregoing findings. The developed SCS1 formulation showed up to 81 fold increase in the solubility and 4.1 fold increase in the dissolution rate of the drug compared to that of the bulk substance. Surprisingly, the developed SCS formulation remained stable for a period of more than one year at accelerated conditions inferred from dissolution studies. It can be concluded that the SCS approach can be used as an alternative contemporary technique to enhance the dissolution rates of many other poorly water-soluble drugs by means of thermal HME processing. SN - 1873-0191 UR - https://www.unboundmedicine.com/medline/citation/28575936/Solid_crystal_suspension_of_Efavirenz_using_hot_melt_extrusion:_Exploring_the_role_of_crystalline_polyols_in_improving_solubility_and_dissolution_rate_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-4931(16)32641-8 DB - PRIME DP - Unbound Medicine ER -