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Acyclovir-Polyethylene Glycol 6000 Binary Dispersions: Mechanistic Insights

Venkateskumar, Krishnamoorthy and Parasuraman, Subramani and Gunasunderi, Raju and Sureshkumar, Krishnan and Nayak, M Muralidhar and Shah, Syed Adnan Ali and Khoo, Khassen and Kai, Heng Wei (2017) Acyclovir-Polyethylene Glycol 6000 Binary Dispersions: Mechanistic Insights. In: AAPS PharmSciTech, 18 (6). pp. 2085-2094. ISSN 1530-9932

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Official URL: https://doi.org/10.1208/s12249-016-0686-9


The dissolution and subsequent oral bioavailability of acyclovir (ACY) is limited by its poor aqueous solubility. An attempt has been made in this work to provide mechanistic insights into the solubility enhancement and dissolution of ACY by using the water-soluble carrier polyethylene glycol 6000 (PEG6000). Solid dispersions with varying ratios of the drug (ACY) and carrier (PEG6000) were prepared and evaluated by phase solubility, in vitro release studies, kinetic analysis, in situ perfusion, and in vitro permeation studies. Solid state characterization was done by powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analysis, and surface morphology was assessed by polarizing microscopic image analysis, scanning electron microscopy, atomic force microscopy, and nuclear magnetic resonance analysis. Thermodynamic parameters indicated the solubilization effect of the carrier. The aqueous solubility and dissolution of ACY was found to be higher in all samples. The findings of XRD, DSC, FTIR and NMR analysis confirmed the formation of solid solution, crystallinity reduction, and the absence of interaction between the drug and carrier. SEM and AFM analysis reports ratified the particle size reduction and change in the surface morphology in samples. The permeation coefficient and amount of ACY diffused were higher in samples in comparison to pure ACY. Stability was found to be higher in dispersions. The results suggest that the study findings provided clear mechanical insights into the solubility and dissolution enhancement of ACY in PEG6000, and such findings could lay the platform for resolving the poor aqueous solubility issues in formulation development.

Item Type: Journal Article
Publication: AAPS PharmSciTech
Publisher: Springer New York LLC
Additional Information: The Copyright of this article belongs to the Springer New York LLC
Keywords: acyclovir; crystallinity; drug-polymer miscibility; solid dispersions; Acyclovir; Animals; Antiviral Agents; Biological Availability; Calorimetry, Differential Scanning; Drug Carriers; Intestinal Absorption; Kinetics; Male; Microscopy, Electron, Scanning; Polyethylene Glycols; Rats; Rats, Sprague-Dawley; Solubility; Spectroscopy, Fourier Transform Infrared; X-Ray Diffraction; aciclovir; macrogol 6000; aciclovir; antivirus agent; drug carrier; macrogol 6000; macrogol derivative; animal experiment; animal tissue; area under the curve; Article; atomic force microscopy; controlled study; differential scanning calorimetry; dispersion; drug absorption; drug penetration; drug release; drug solubility; drug stability; image analysis; in vitro study; infrared spectroscopy; intestine absorption; male; mean dissolution time; mean residence time; morphology; nonhuman; nuclear magnetic resonance; particle size; priority journal; rat; reduction (chemistry); scanning electron microscopy; solid state; surface property; X ray diffraction; animal; bioavailability; drug effects; kinetics; metabolism; physiology; procedures; solubility; Sprague Dawley rat; synthesis
Department/Centre: Others
Date Deposited: 17 Jun 2022 07:29
Last Modified: 17 Jun 2022 07:29
URI: https://eprints.iisc.ac.in/id/eprint/73514

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