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RESEARCH JOURNAL OF PHARMACY AND TECHNOLOGY
Year : 2020, Volume : 13, Issue : 12
First page : ( 5979) Last page : ( 5986)
Print ISSN : 0974-3618. Online ISSN : 0974-360X.
Article DOI : 10.5958/0974-360X.2020.01043.4

Enhanced solubility of microwave-assisted synthesized acyclovir Co-crystals

Bhandare Richie1*, Londhe Vaishali2*, Ashames Akram1, Shaikh Nadeem2, Alabdin Sham Zain1

1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman, United Arab Emirates.

2SVKM's NMIMS, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, Vile Parle [W], Mumbai, Maharashtra, India.

*Corresponding Author E-mail: r.bhandareh@ajman.ac.ae; vaishali.londhe@nmims.edu

Online published on 15 February, 2021.

Abstract

This study aimed to enhance the kinetic solubility of ACV by using microwave-assisted technique to form ACV co-crystals and overcome its limited aqueous solubility. Co-crystallization is one of the commonly used techniques to improve the dissolution rates of active pharmaceutical ingredients (APIs). Acyclovir (ACV) has a limited efficacy due to its low oral bioavailability resulted from its poor aqueous solubility and permeability. Acyclovir co-crystals were formulated by microwave assisted solvent extraction (MASE) in equimolar ratio of 1:1 with different co-formers. Physical and structural characterization by differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), and Fourier transform infrared (FTIR) spectroscopy were performed. Further evaluation of the co-crystals solubility, dissolution rate and content were carried out using the ultraviolet (UV) spectrophotometry. Co-crystals of acyclovir and tartaric acid (ACV-TA) in equimolar ratio of 1:1 produced by MASE using the glacial acetic acid as a solvent were more soluble compared to plain drug. The dissolution rate was increased from only 59.0% of pure acyclovir up to 85.0% of ACV co-crystals within 1 hour. DSC and PXRD patterns of co-crystals were distinguished from that of individual components. The UV-spectroscopic analysis represented 62.5% of acyclovir in the co-crystals, which was directly related to the theoretical percentage of the drug and its co-former (ACV: 60.01%, TA: 39.99%). This study revealed that the optimal ratio of the ACV-TA co-crystal is 1:1, which was successfully prepared using MASE technique. This method provides a promising alternative for enhancing the solubility of acyclovir with ultimately less time and solvent consumption.

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Keywords

Co-crystals, Aqueous solubility, Dissolution rate, Acyclovir, Co-former, Microwave, Solvent evaporation, FTIR, Spectrophotometer, PXRD, DSC.

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