Preparation and characterization of nanoparticles of carboxymethyl cellulose acetate butyrate containing acyclovir

Venkata Bharadwaz Vedula,Emil Joseph,Sonal Mazumder,Maulick Chopra

doi:10.1007/s13204-015-0421-y

Venkata Bharadwaz Vedula, Emil Joseph + Show 2 more

Open Access

https://doi.org/10.1007/s13204-015-0421-y

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Abstract

Nanoparticles of carboxymethyl cellulose acetate butyrate complexed with the poorly soluble antiviral drug acyclovir (ACV) were produced by precipitation process and the formulation process and properties of nanoparticles were investigated. Two different particle synthesis methods were explored—a conventional precipitation method and a rapid precipitation in a multi-inlet vortex mixer. The particles were processed by rotavap followed by freeze-drying. Particle diameters as measured by dynamic light scattering were dependent on the synthesis method used. The conventional precipitation method did not show desired particle size distribution, whereas particles prepared by the mixer showed well-defined particle size ~125–450 nm before and after freeze-drying, respectively, with narrow polydispersity indices. Fourier transform infrared spectroscopy showed chemical stability and intactness of entrapped drug in the nanoparticles. Differential scanning calorimetry showed that the drug was in amorphous state in the polymer matrix. ACV drug loading was around 10 wt%. The release studies showed increase in solution concentration of drug from the nanoparticles compared to the as-received crystalline drug.

Highlights

There are many options for increasing the bioavailability of poorly soluble drugs like adding of ionized salts, solid dispersions, micronization technique and soft gel technology (Elaine et al 2003)
We investigated how different particle processing schemes affected particle properties, notably particle size and drug loading
These processing approaches included nanoparticle preparation by (1) simple precipitation followed by rotavap, centrifugation and drying in oven and (2) rapid precipitation in a mixer followed by rotavap and freezedrying

Summary

Introduction

There are many options for increasing the bioavailability of poorly soluble drugs like adding of ionized salts, solid dispersions, micronization technique and soft gel technology (Elaine et al 2003). These methods have their own limitations in terms of drug-loading capacity, toxicity, biodegradability, large dosages and environmental considerations. Herpes simplex virus-1, the primary virus of all the 25 subfamilies of HV, is the primary cause for genital infections, corneal opacities, shingles and chickenpox in human beings. Acyclovir (ACV) was approved as drug of choice for treatment of infections caused by this virus (Antona et al 1994), Fig. 1.

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