Affiliation:
1. Institute of Pharmacy and Technology, Salipur, Cuttack 754202, Odisha, India
2. Department of Pharmaceutical Chemistry, Global Institute of Pharmaceutical Education and Research, Affiliated to Uttarakhand Technical University, Kashipur 244713, India
Abstract
Objective:
Literature study revealed the poor mechanical strength of chitosan-based
microparticles. Our research aimed at developing sufficient strength of microparticle with a
suitable concentration of chitosan and non-ionic surfactants such as poloxamer-188 (pluronic). It
also aimed to develop and study the effect of variables for prepared microparticles utilizing insilico
screening methodology, such as reduced factorial design, followed by optimization.
Methods:
Preliminary trial batches were prepared with variable concentration of chitosan and
poloxamer-188 utilizing cross-linked ion-gelation technique. A 20% w/v sodium citrate solution
was used as a cross-linking solution. The resolution-IV of 24-1 reduced factorial design was
selected to screen the possible and significant independent variables or factors in the dosage form
design. A total number of eight runs were suggested by statistical software and responses were
recorded. The responses such as spreadability, pH, viscosity and percentage of drug released at 12
h were considered in the screening study. Based on the result, selected factors were included in the
optimization technique, including graphical and numerical methods.
Results:
The signified factors based on reduced two-level factorial screening design with
randomized subtype, were identified by Half-normal and Pareto chart. Mathematical fitting and
analysis were performed by the factorial equation during the optimization process. The validation
and fitting of models were suggested and evaluated by p-value, adjusted R2, and predicted R2 values.
The significant and non-significant terms were evaluated, followed by finding the optimal
concentration and region with yellow color highlighted in an overlay plot. Based on the data obtained
by the overlay study, the final formulation batch was prepared and the observed value was found to be
pretty much nearer as compared to predicted values. Drug-polymer interaction study included
attenuated total reflectance, differential scanning calorimetry, and X-Ray diffraction study.
Conclusion:
The principal of the study design was based on finding the prefixed set parameter
values utilizing the concept of in-silico screening technique and optimization with a minimal
number of trials and study expenses. It concluded that Poloxamer-188 (0.94%), chitosan (2.38%),
swelling time (1.81 h), and parts of chitosan (78.51%) in a formulation batch would fulfill the
predetermined parameter with specific values.
Publisher
Bentham Science Publishers Ltd.
Subject
Organic Chemistry,Computer Science Applications,Drug Discovery,General Medicine
Cited by
4 articles.
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