Abstract
Objectives: Aim of present work is to prepare and evaluate Sustained release microspheres of Acebrophylline for treatment of Asthma.
 Experimental work: In present investigation, attempt was made to prepare sustained release microspheres of Acebrophylline with different polymer ratio using Ionic gelation method. Drug- excipient compatibility studies were performed by FTIR. The best suited Microspheres formulation was found on the basis production yield, entrapment efficiency and in vitro release study. Optimized batch of microspheres (B2) was characterized for FTIR, DSC, and SEM analysis. The drug release data of optimized batch was fitted into different release kinetic models. The optimized batch of microspheres (B2) was subjected for the short term stability study at 40 ± 2°C with RH of 75% for a period of 1 month.
 Results and discussion: There was no interaction found between drug and excipients. Sodium alginate (2%) concentration, Eudragit RS-100 (1:2) ratio gave highest sustainable property and CaCl2 (2.5%) concentration had a good cross linking property. This observation done on the basis of production yield, entrapment efficiency and In vitro release study. The Microspheres prepared from Ionic gelation method had Drug : Eudragit RS100 (1:2), 2 % Sodium alginate and 2.5 % CaCl2 (B2) give 99.2 % drug release over the periods of 12 hr. The drug release from optimized microspheres formulation (B2) follows first order release kinetic. DSC study showed the melting behavior of drug present into microspheres. SEM studies showed that optimized microspheres were spherical and rough surface. Stability study proved that optimized formulation (B2) was stable.
 Conclusion: Drug: Polymer ratio and Volume of CaCl2 had significant effect on % Entrapment efficiency and Drug release. From the Scanning Electron Microscopy (SEM) study observed that microspheres was spherical and rough surface. Non Fickian diffusion was the mode of drug release from Acebrophylline- loaded microspheres. After stability study no physical changes & almost same drug release was observed in microspheres. Hence, the formulation B2 was stable.
Highlights
The goal in designing sustained delivery systems is to reduce the frequency of the dosing or to increase effectiveness of the drug by localization at the site of action, reducing the dose required or providing uniform drug delivery
The results revealed that the drug and polymers were satisfactorily compatible, without any significant changes in the chemical nature of the drug
Microspheres were prepared by different techniques like Ionic gelation and Emulsification crosslinking method
Summary
The goal in designing sustained delivery systems is to reduce the frequency of the dosing or to increase effectiveness of the drug by localization at the site of action, reducing the dose required or providing uniform drug delivery. Sustained release dosage form is a dosage form that release one or more drugs continuously in a predetermined pattern for a fixed period of time, either systemically or to a specified target organ.[1]sustained release dosage forms provide a better control of plasma drug levels, less dosage frequency, less side effect, increased efficacy and constant delivery.[2]. These systems provide a slow release of drug over an extended period of time and can provide some control, whether this be of a temporal or spatial nature, or both, of drug release in the body, or in other words, the system is successful at maintaining constant drug levels in the target tissue or cells. There are two types of micro particles F1) Microcapsules: Micrometric Reservoir systems 2) Microspheres: Micrometric Matrix systems
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