Evaluation and controlled release characteristics of modified xanthan films for transdermal delivery of atenolol.
The present study was performed to evaluate the possibility of using modified xanthan films as a matrix system for transdermal delivery of atenolol (ATL), which is an antihypertensive drug. Acrylamide was grafted onto xanthan gum (XG) by free radical polymerization using ceric ion as an initiator. Fourier transform infrared spectroscopy and differential scanning calorimetry indicated the formation of the graft copolymer. The obtained graft copolymer was loaded with ATL and films were fabricated by solution casting method for transdermal application. Various formulations were prepared by varying the grafting ratio, drug loading, and different penetration enhancers. The formulations prepared were characterized for weight, thickness uniformity, water vapor transmission rate, and uniformity in drug content of the matrix. All the thin films were slightly opaque, smooth, flexible, and permeable to water vapor, indicating their permeability characteristics suitable for transdermal studies. Fourier transform infrared spectroscopy and differential scanning calorimetry studies indicated no significant interactions between drug and polymer. Drug is distributed uniformly in the matrix but showed a slight amorphous nature. Drug-loaded films were analyzed by X-ray diffraction to understand the drug polymorphism inside the films. Scanning electron microscopic studies of the placebo and drug-loaded films demonstrated a remarkable change in their surface morphology. The skin irritation tests were performed in mice and these results suggested that both placebo and drug-loaded films produced negligible erythema and edema compared to formalin (0.8% v/v) as the standard irritant. The in vitro drug release studies were performed in phosphate buffer saline using a Keshary-Chien diffusion cell. Different formulations were prepared and variations in drug release profiles were observed. Release data were analyzed by using the Ritger and Peppas equation to understand the mechanism of drug release as well as the estimation of n values, which ranged between 0.41 and 0.53, suggesting a Fickian diffusion trend.
Mundargi
Raghavendra C
RC
Department of Chemistry, Center of Excellence in Polymer Science, Karnatak University, Dharwad, India.
Patil
Sangamesh A
SA
Agnihotri
Sunil A
SA
Aminabhavi
Tejraj M
TM
D000180:Acrylic Resins / Q000008:administration & dosage; D000279:Administration, Cutaneous; D000818:Animals; D001262:Atenolol / Q000008:administration & dosage* / Q000737:chemistry; D003692:Delayed-Action Preparations; D051379:Mice; D011135:Polysaccharides, Bacterial / Q000008:administration & dosage*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction; D000099166:Polyacrylamides
D000180:Acrylic Resins; D001262:Atenolol; D003692:Delayed-Action Preparations; D011135:Polysaccharides, Bacterial; D000099166:Polyacrylamides; C002563:xanthan gum