The Relationship between Elasticity of Polymeric Gels and the In vitro Release of Medicaments (original) (raw)
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Relation between structural and release properties in a polysaccharide gel system
Biophysical Chemistry, 2007
The potential utility of κ-carrageenan gels for preparing drug release devices is here shown. Structural properties of κ-carrageenan gels prepared with different salt composition and containing Ketoprofen sodium salt, as model drug, have been evaluated with static light scattering and rheological measurements. These properties have been correlated with release profiles in vitro at pH 5.5. Release properties from gelled matrices have been compared with those obtained by two commercial products containing the same drug. Results show that: i) in this system it is possible to easily control the gel texture by using different cationic concentration; ii) the kinetics of drug release by κ-carrageenan gels are dependent on the structural properties of matrices; iii) in the typical interval time used in classical local applications, all gel samples release the loaded drug almost completely, at difference with the commercial products. All these findings can provide useful suggestions for the realization of classical topical release systems.
International Journal of Applied Pharmaceutics, 2019
Objective: Super porous hydrogels (SPHs), a novel drug delivery system can be developed to retain drugs in the gastric medium. The aim of the present investigation was to prepare superporous hydrogels (SPHs) of Atenolol to release the drug in sustained manner in the gastric environment and study the effect of two grades of hydroxyl methyl cellulose along with Carbopol 971p on the physico mechanical properties and drug release kinetics of the formulations. Methods: Superporous hydrogels of Atenolol were prepared with two grades of Hydroxy Propyl Methyl Cellulose (HPMC K100M and HPMC K15 M) along with Carbopol 971p the structural morphology of hydrogel was observed by Scanning Electron Microscopy. Study on Physico mechanical characteristics and drug release were done. Results: Scanning Electron microscopy studies of the formulations revealed the presence of large number of pores in different size ranges like 1 µm, 2 µm, 10 µm, confirming the formulations as superporous hydrogel. A correlation had been found between porosity, density and % swelling index. The drug release data from the formulations obeyed Higuchi and Korsmeyer-Peppas kinetics. Further, the data were fitted to the Kopcha model for confirming drug release by a combination of diffusion-controlled and chain relaxation-swelling mechanism. Conclusion: Among the six formulations, where HPMC K15 M and HPMC K100 M both were present, the gel became more hydrophobic and retarded the release of drug. From the drug release kinetics data, it can be concluded that the diffusion mechanism predominated the drug release process, leading to quasi diffusion and Fickian diffusion mechanism.
IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM Original Article
International Journal of Applied Pharmaceutics, 2018
The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach. Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3 Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study. Conclusion: This study showed the formulation of Na alginate with GG and CaCO3
DEVELOPMENT AND EVALUATION OF HYDROGEL OF AN ANTI-FUNGAL DRUG Original Article
International Journal of Pharmacy and Pharmaceutical Sciences, 2023
Objective: Topical gel preparations are used for application on skin or to certain mucosal surfaces for local action or for their emollient or protective action. Topical delivery of drugs can be achieved by incorporating drugs into the hydrogel matrix for effective delivery of drugs, thus avoiding first-pass metabolism and for increased local action in pain management and skin diseases. Methods: Hydrogel is a network of polymer chains that are hydrophilic, sometimes found as a colloidal gel in which water is the dispersion medium. Miconazole nitrate (MN) is a broad-spectrum antifungal agent of the imidazole group. It has been selected as a model drug for the preparation of hydrogel. For the preparation of hydrogel, Carbopol of different grades like 934p, 971p, and 974p have been selected. Drug-polymer interaction has been carried out by FT-IR spectroscopy. Standard curve of miconazole nitrate was prepared in phosphate buffer pH 5.5 and 7.4. Physico-chemical characteristics of the hydrogel, like pH, viscosity and % swelling index, were studied. % cumulative drug permeation study through dialysis membrane was done in phosphate buffer pH 7.4. Results: The results were found to be satisfactory. Carbopols have been used in different ratios to get a number of formulations. Out of these, nine formulations have been chosen by their satisfactory physicochemical characteristics and used for the study. The average pH, viscosity, % swelling index and drug content were found to be 7.36, 1.09 x 100 cps, 23.1 and 98.36 %, respectively. Drug permeation kinetics through the dialysis membrane has been done in a Franz diffusion cell at phosphate buffer pH-7.4. The permeation of Miconazole Nitrate through the dialysis membrane was maximum in F1 and minimum in F9. The drug permeation through the dialysis membrane followed zero-order kinetics. Conclusion: A sharp correlation between the % swelling index and the Cumulative % of drug permeated through the dialysis membrane has been found. With the increase in the % swelling index over a period of 6 h the permeation decreased; thus, the swelling of the formulations is responsible to inhibit the permeation of Miconazole Nitrate through the skin.
In Situ Gel as Platform for Ketoconazole Slow Release Dosage Form
International Journal of Applied Pharmaceutics
Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration re...
Comparative Evaluation of HPMC, PVA and Gelatin as Matrices for Controlled Release Drug Delivery
Stamford Journal of Pharmaceutical Sciences, 2010
The present study was undertaken to compare three different polymeric gums- HPMC, PVA and gelatin as controlled release matrices. Diclofenac sodium, a potent analgesic, was used as the model drug. Different ratio of HPMC, PVA and gelatin were incorporated into the lactose loaded Diclofenac tablet to explore their impact on drug release. Matrix tablets of Diclofenac were prepared by using individual polymer with magnesium stearate and aerosil by direct compression process at 5 ton pressure. The release of drug from these matrices was studied over 2 hrs in acidic media where insignificant release was observed. Then, the same formulations were studied over 8 hours in buffer media of pH 6.8 at a temperature of 37± 0.5°C. Statistically significant differences in drug release profile was found among the tablets prepared from different matrices. The study revealed that the average % release of drug from different types of polymer loaded matrix tablet varied with the ratio of different poly...