Famotidine microspheres reconstituted with floating in situ gel for stomach-specific delivery: Preparation and characterization

Singhavi, Dilesh J.; Pundkar, Rashmi S.; Khan, Shagufta

doi:10.1016/j.jddst.2017.07.017

Cited by 14 publications

(8 citation statements)

References 61 publications

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“…Characterization of floating in-situ gel [19][20][21][22][23] : Physical appearance: General appearance of formulation like colour, odour was observed.…”

Section: Drug Excipient Compatibility Studymentioning

confidence: 99%

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Formulation and Evaluation of Floating In-Situ Gel of Nicardipine Hydrochloride

Patel¹,

Desai²,

Jain³

et al. 2022

J. Drug Delivery Ther.

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The present research work aimed to formulate and evaluate a gastro retentive in situ gelling system of Nicardipine Hydrochloride using Sodium Alginate as gelling polymer, HPMC K100M as release retard polymer, calcium carbonate as a cross-linking agent, and tri-sodium citrate as fluidity enhancer agent to treat hypertension. The mechanism for the floatation was based on ionic cross-linking. Several evaluation tests were carried out for pre and final formulation evaluation. Based on the outcomes white-colored, viscous solution of uniform consistency was obtained. Batch B1 was very well prepared for the ability to control long-term drug release. The drug content was found to be > 97 %, the viscosities were in the acceptable range suitable for swallowing, and pH was found to be in the range of 7.33 – 7.68 which was compatible with oral digestion. Design expert 13 Software was used to derive results of interaction and responses based on the concentration of polymer and statistical analysis. The optimized formulation i.e., Batch B1 (0.6 % w/v and 0.5 % w/v HPMC K100M) showed a slow drug release of 96.44 % up to 12 hours. The best fit model for the drug release followed the Higuchi model which explained that the drug release occurred by the Fiskian mechanism i.e., a combination of both diffusion and erosion. The in-situ gel prepared can ultimately provide prolonged release, enhance the bioavailability of the drug and increase patient compliance. Keywords: - In situ gel, Ionic cross linking, Sodium alginate, HPMC K100M, Nicardipine Hydrochloride.

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“…Characterization of floating in-situ gel [19][20][21][22][23] : Physical appearance: General appearance of formulation like colour, odour was observed.…”

Section: Drug Excipient Compatibility Studymentioning

confidence: 99%

“…R 2 is a statistical measure of how close the data are to the fitted regression line. The value close to 1 was considered to be the most preferred one [19][20][21]24 .…”

Section: Drug Release Kineticsmentioning

confidence: 99%

Formulation and Evaluation of Floating In-Situ Gel of Nicardipine Hydrochloride

Patel¹,

Desai²,

Jain³

et al. 2022

J. Drug Delivery Ther.

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“…Where, Wt is the total initial amount of 5-FU incorporated during formulation development, and Wf is the amount of free drug in the solution after formulating the drug entrapped microspheres (Singhavi et al, 2017).…”

Section: Estimation Of Drug Entrapment Efficiency (Ee)mentioning

confidence: 99%

Polymeric Microsphere Formulation for Colon Targeted Delivery of 5-Fluorouracil Using Biocompatible Natural Gum Katira

Karan

Choudhury

Chakra

et al. 2019

Asian Pac J Cancer Prev

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Controlled release delivery system of chemotherapeutic agents at the site of colon endorses modern drug-entrapped delivery tools, which release the entrappedagents at a controlled rate for anextended period providing patient compliance and additional protection from the degradinggastric environment. Thus, the present study was aimed to develop and optimize a novel polymeric microsphere of 5-fluorouracil (5-FU) using natural gum katira to obtain an optimal therapeutic response at the colon. Due course of experimentation, in-vivo safety profile of the gum katira in an animal model was established. Modified solvent extraction/evaporation technique wasemployed to encapsulate 5-FU in the natural polymeric microsphere and was characterized using in-vitro studies to investigate particle size, morphology, encapsulation efficiency and release of the drug from developed formulation. Formulated and optimized polymeric microsphere of 5-FU using gum katira polymer own optimal physicochemical characteristics with a fine spherical particle with size ranged from 210.37±7.50 to 314.45±7.80 µm.Targeted microsphere exhibited good cytotoxicity and also has high drug entrapment efficiency, and satisfactory release pattern of the drug within a time frame of 12 h. Finally, we foresee that the optimized polymeric gum katiramicrosphere of 5-FU could be a promising micro-carrier for efficient colon drug targeting delivery tool with improved chemotherapeutic efficacy against colon cancer.

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“…Particle size of microspheres formed majorly depends on the ascorbic acid concentration and degree of deacetylation. Chitosan with higher degree of deacetylation makes it susceptible to provides more number of effective binding sites for the ionic interaction with ample positive charge due to amino groups that protonated in the acidic environment 36 . Whereas the increment in the concentration of ascorbic acid in which chitosan was dissolved also enhancing the ability of chitosan to form linkage with STPP anion hence microspheres decrease in particle size (Table 1).…”

Section: Preparation Of Carrier Systemmentioning

confidence: 99%

Therapeutic Management of Pulmonary Tuberculosis by Mannosylated Chitosan Ascorbate Microspheres: Preparation and Characterization

Bagre

Lariya

Kori

2019

J. Drug Delivery Ther.

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Objective: In this study, biodegradable Chitosan Ascorbate Microsphere (CAMs) and mannosylated chitosan ascorbate microsphere (m-CAMs) prepared for targeting towards alveolar macrophages to treatment of pulmonary tuberculosis. Significance: Ascorbic acid is an antioxidant and reported killing effect on mycobacterium by induces fenton reaction. This study enlightens the possible benefits of adding antioxidant properties of ascorbic acid with chitosan microsphere to an anti-tuberculosis regimen and mannosylation of microsphere significantly induce the targetability of antitubercular drug to alveolar macrophages. Methods: CAMs prepared by firstly salification of chitosan by ascorbic acid then ionic gelation with STPP and m-CAMs prepared by incubation method and purified for further studies. The physicochemical, in vitro and in vivo characterizations of both formulations were carried out. Results: The size of microspheres (both CAMs and m-CAMs) were found to be in range of 3.40-4.81µm. Evident changes were observed in crystallinity and structure of both carrier systems and depicted by Fourier transform infrared (FTIR), Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. In vitro lung deposition study of microspheres showed favourable aerodynamic properties for deep lung delivery (MMAD 2.0- 3.8 μm) and, thus, show potential for an application as inhalable tuberculosis therapy. The drug release showed the biphasic pattern of release, i.e., initial burst (30-45% up to 8 h) followed by a slower sustained release pattern (more than 80% up to 72 h) in both simulated lung fluids. Optimized formulations exhibited lower cytotoxicity and bio distribution studies demonstrated the efficiency of m-CAMs for spatial delivery of INH to alveolar tissues. CAMs and m-CAMs evidenced minor cytotoxicity on lung epithelial cells (A549 cell lines). Conclusion: m-CAMs thus has a promising potential to be explore as an effective carrier system for delivery of antitubercular drugs regimen. Key words: Targetability, alveolar macrophage, lung cancer A549 cells

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Famotidine microspheres reconstituted with floating in situ gel for stomach-specific delivery: Preparation and characterization

Cited by 14 publications

References 61 publications

Formulation and Evaluation of Floating In-Situ Gel of Nicardipine Hydrochloride

Formulation and Evaluation of Floating In-Situ Gel of Nicardipine Hydrochloride

Polymeric Microsphere Formulation for Colon Targeted Delivery of 5-Fluorouracil Using Biocompatible Natural Gum Katira

Therapeutic Management of Pulmonary Tuberculosis by Mannosylated Chitosan Ascorbate Microspheres: Preparation and Characterization

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