Author(s): Richie Bhandare, Vaishali Londhe, Akram Ashames, Nadeem Shaikh, Sham Zain Alabdin

Email(s): r.bhandareh@ajman.ac.ae , vaishali.londhe@nmims.edu

DOI: 10.5958/0974-360X.2020.01043.4   

Address: Richie Bhandare1*, Vaishali Londhe2*, Akram Ashames1, Nadeem Shaikh2, Sham Zain Alabdin1
1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman, UAE.
2SVKM’s NMIMS, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, Vile Parle [W], Mumbai, Maharashtra, India.
*Corresponding Author

Published In:   Volume - 13,      Issue - 12,     Year - 2020


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.


Cite this article:
Richie Bhandare, Vaishali Londhe, Akram Ashames, Nadeem Shaikh, Sham Zain Alabdin. Enhanced Solubility of Microwave-assisted Synthesized Acyclovir Co-crystals. Research J. Pharm. and Tech. 2020; 13(12):5979-5986. doi: 10.5958/0974-360X.2020.01043.4


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