Development of Acyclovir Loaded β‐Cyclodextrin‐g‐Poly Methacrylic Acid Hydrogel Microparticles: An In Vitro Characterization

Abstract

In this work, successful efforts have been performed for solubility enhancement of acyclovir. pH‐sensitive β‐Cyclodextrin‐g‐poly methacrylic acid (MAA) hydrogel microparticles were developed. β‐Cyclodextrin, MAA, N,N‐methylene bisacrylamide were used as polymer, monomer, and cross‐linker, respectively. Nine different formulations (BM‐1 to BM‐9) were prepared by aqueous free radical polymerization. Developed microparticles were characterized for FTIR, Differential Scanning Calorimetry/Thermo Gravimetric Analysis, PXRD, energy‐dispersive x‐ray spectroscopy, SEM, TEM, optical microscopy, zeta sizer, percent equilibrium swelling (%ES), solubility studies, and in vitro drug release studies. Higher swelling results (83.68%) were obtained at pH 7.4 in less than 3 h. Porous surfaces with drug were seen in TEM images. Maximum release was observed at pH 7.4 (89.51%). Solubility enhancement was 7.38‐fold in water as compared to pure acyclovir. Thermal stability of grafted microparticles was increased up to 440.13°C. A potential approach for solubility enhancement was successfully developed.

Development and <i>in vitro</i> characterization of 5-flurouracilloaded, colon-targeted drug delivery system

“…This technique also serves to confirm sucessfull loading of active moeity within the carrier system [15].…”

“…The IR spectra were obtained for 5-FU, chondroitin sulphate and PVA; and for physical mixtures of drug and polymers, unloaded chondroitin sulphate-grafted PVA miCAPs, and the 5-FUmiCAPs using ATR-FTIR (Tensor 27). The range of wavelengths used for the scan was 500 − 4000 cm −1 at a resolution of 4 cm −1 [15].…”

“…Prior to sample application, the pans were subjected to tarring. With the reference pan empty, the sample pan was halffilled, and heat was applied to the furnace, raising the temperature to 450 °C at a flow rate of 15°C/min in a nitrogen medium [15]. The temperature at which melting of the raw materials and miCAPs occurred as well as the temperature for entire combustion was calculated to assess the stability of the miCAPs.…”

“…In the assessment of internal morphology, the miCAPs were embedded in acrylate glue, dried and cut into slices which were placed on scanning stubs to obtain the internal SEM images [15].…”

“…Particle size analyzer (Zeta-sizer Nano-series ZEN3600, Malvern Instruments Ltd. with software DTS-nano, Kingdom) was used for the estimation of the particle sizes of the miCAPs [15].…”