Purpose: Various floating and pulsatile drug delivery systems suffer from variations in the gastric transit time affecting the bioavailability of drugs. The objective of the study was to develop Pantoprazole Sodium (PAN) microballoons that may prolong the gastric residence time and could enhance the drug bioavailability.Methods: Microballoons were prepared using Eudragit®L100 by adopting emulsion solvent diffusion method with non-effervescent approach, in vitro studies were performed and the in vivo evaluation was carried out employing ethanol induced ulceration method. Optimization and validation were carried out through Design Expert® software.Results: The results demonstrate an increase in percentage yield, buoyancy, encapsulation efficacy and swelling. Particles were in the size range 80-100 µm following zero order release pattern. SEM study revealed their rough surface with spherical shape, internal cavity and porous walls. DSC thermo gram confirms the encapsulation of drug in amorphous form. Significant anti ulcer activity was observed for the prepared microballoons. The calculated ulcer index and protection were 0.20±0.05 and 97.43 % respectively for LRS-O (optimized formulation).Conclusion: This kind of pH dependent drug delivery may provide an efficient dosage regimen with enhanced patient compliance.
Drugs with lower bioavailability need repeated dosing to reach the minimum effective therapeutic concentration in plasma. In order to retain the drug in upper part of gastro intestinal tract (GIT) which is the major absorption window for majority of drugs and also to have localized effect many advances in drug delivery were made. Researchers mainly emphasize on to get patient compliance by formulating single dose, targeted and minimal side effects dosage form. The design must give constant drug release for longer time period that could be achieved through proper selection of polymers. These approaches in dosage design may also be advantageous for local action, to prevent drug degradation, delivery of gastro-irritant, narrow absorption window drugs and to get pH dependent release throughout the GIT. Polymethacrylate polymers in different ratios are available for the above objective as they are inert materials, could stay for longer time and are resistant to body fluids. This review also discusses the physicochemical properties of different available grades along with their glass transition temperatures (Tg).
The discovery of biological clock has changed many established concepts and hypotheses in pharmacology and medicine. Diseases borne due to disturbances or deregulation of biological clock are set right only by setting the clock right. There are many natural and life style factors which deregulate the clock. Recently many chronotherapeutic drugs were discovered and tested this review throw light on such problems.
Background: Microspheres are controlled drug delivery systems (CDDS) because they have the potential to encapsulate various drugs, nucleic acids, and proteins. Their benefits include biocompatiblity, greater bioavailability, and controlled release. Presently, existing antiulcer agents suffer from severe side effects which restricted their utility and encouraged the requirement of a harmless and proficient new antiulcer agent. The rationale of the present research work was to absorb the drug in the stomach for better antiulcer potential and fewer side effects. Objective: The rationale of the current investigational effort is to prepare and examine floating microspheres using berberine hydrochloride to increase gastric retention without interaction with the mucosa inside the stomach. Methods: The capillary extrusion technique was used with the aid of chitosan, a polymer in addition to sodium lauryl sulphate, a crosslinking agent. Scanning electron microscopy characterized the surface morphology of the prepared microspheres. The effects of polymeric concentration as well as the concentration of cross-link agent on percent yield, in vitro floating behavior, and in vitro drug release were efficiently assessed. Results: Diffusion has been observed as a popular mechanism for most launches. Prolonged drug release (12 hrs) has been seen in the prepared microspheres and they also remained buoyant for around 10 hrs. In vivo evaluation study was successfully performed. From the values of ulcer indexes for various groups, percentage protection was determined. The treatment group (F-2 formulation) showed the maximum percentage protection of 97.29%. Conclusion: The prepared floating microspheres can thus persuade potential candidates to be adaptable to any intra-gastric conditions for multiple-unit delivery devices.
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