Influence of polymer ratio and surfactants on controlled drug release from cellulosic microsponges

Shahzad, Yasser; Saeed, Soobia; Ghori, Muhammad Usman; Mahmood, Tariq; Yousaf, Abid Mehmood; Jamshaid, Muhammad; Sheikh, Rizwan; Rizvi, Syed A. A.

doi:10.1016/j.ijbiomac.2017.11.089

Cited by 48 publications

(27 citation statements)

References 32 publications

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“…In comparison multi-unit dosage forms such as microparticles are beneficial as they can prolong GRT which leads to improved bioavailability [3] and avoids dose dumping, which is often associated with the single-unit delivery systems such as tablets, capsules etc. [4]. Microparticles are small sized multi-unit dosage forms as compared to single-unit systems; the presence of food in gastrointestinal tract (GIT) and GIT motility pose fewer effects on transport of these particles.…”

Section: Introductionmentioning

confidence: 99%

Probing the effect of various lipids and polymer blends on clopidogrel encapsulated floating microcarriers

et al. 2019

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Background Clopidogrel (CLOP) is an antiplatelet drug with poor solubility in intestinal fluid, which limits its bioavailability after oral administration. Objectives Current study focuses on developing site-specific floating microcarriers of CLOP using solvent diffusion evaporation method (SDEM) for retaining the drug in the stomach, thus improving the solubility of drug for better absorption. Methods SDEM was employed to formulate floating microcarriers using lipidic excipients, namely Gelucires (GL) to impart floating properties, in combination with ethyl cellulose as release retarding polymer. Results Prepared particles were 169 ± 6 μm to 375 ± 13 μm in size, whilst encapsulation efficiency was ranged from 39.6 ± 0.60% to 96.50 ± 3.50%. Electron micrographs depicted discrete spherical microcarriers with porous structure, which amplified with increasing HLB value of GL and concentration of Eudragit E100. FTIR study confirmed absence of major drug polymer interactions while DSC and XRD studies revealed the presence of non-crystalline nature of drug in all formulations. Drug release at pH 1.2 enhanced more than 2-folds with increasing HLB value with 32% cumulative drug release for GL 43/01 and 69% for GL 50/13. More interestingly, adding various proportions of Eudragit E100 to GL 43/01 based formulations resulted in increased drug release as high as 71%. In all formulations, the drug release followed diffusion dependent process. Conclusion It is envisaged that this formulation strategy for CLOP is promising and could possibly be tested in future for its in vivo performance.

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Section: Introductionmentioning

confidence: 99%

Probing the effect of various lipids and polymer blends on clopidogrel encapsulated floating microcarriers

et al. 2019

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“…Lornoxicam-laden cellulosic microsponges were synthesized using a slightly modified quasi emulsion-solvent diffusion method as reported previously by our research group ( Shahzad et al, 2018 ). Briefly, matrix forming polymers including EC:HPMC at a weight ratio of 9:1 w/w were dissolved in 6 mL of organic phase (internal phase) consisted of 5 mL of dichloromethane and 1 mL of ethanol.…”

Section: Methodsmentioning

confidence: 99%

“…We have recently reported a new microsponge delivery system made of a combination of hydrophilic and hydrophobic polymers as a matrix components. These microsponges acted like a dry-sponge with a capability of high loading and controlled release of ketoprofen in a sustained fashion for upto 8 h ( Shahzad et al, 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Formulation and characterization of lornoxicam-loaded cellulosic-microsponge gel for possible applications in arthritis

He¹,

Majid

Maqbool

et al. 2020

Saudi Pharmaceutical Journal

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Rheumatoid arthritis (RA) is an autoimmune disease associated with severe joint pain. Herein, we report lornoxicam loaded cellulosic microsponge gel formulation with sustained anti-inflammatory effects that are required to manage arthritic pain. The microsponges were formulated using quasi emulsion-solvent diffusion method employing four different surfactant systems, namely polyvinyl alcohol (PVA), Tween80, Gelucire 48/16 and Gelucire 50/13. All the lornoxicam loaded microsponge formulations were extensively characterized with a variety of analytical tools. The optimized microsponge formulation was then converted into gel formulation. The lornoxicam loaded microsponge gel formulation had adequate viscosity and sufficient pharmaceutical properties as confirmed by the texture analysis and the drug release followed Super case II transport. It is noteworthy that we described the preparation of a new cellulosic polymers based microsponge system for delivery of lornoxicam to provide quick as well as lasting (sustained) anti-inflammatory effects in rats using carrageenan induced rat paw edema model. We were able to demonstrate a 72% reduction in inflammation within 4 h using the optimize transdermal gel formulation utilizing Transcutol P as permeation enhancer and with the aid of skin micro-piercing by microneedles, hence, demonstrating the potential of this microsponge gel formulation in arthritis management.

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“…A super case II transport is achieved if the n value is greater than 0.89. Super case II transport involves release of the drug through combined diffusion and polymer erosion mechanisms [36,37]. The corresponding n values for F1, F3 and F4 suggested a non-Fickian diffusion of nizatidine molecules from the polymer matrix.…”

Section: Drug Release Kineticsmentioning

confidence: 99%

Relevancy of Nizatidine Release from Floating Tablets with Viscosity of Various Cellulose Ethers

Shahzad¹,

Ibrar²,

Hussain³

et al. 2019

Sci

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Nizatidine is a gastroprotective drug with a short biological half-life and narrow absorption window. This study aimed at developing floating tablets of nizatidine using various HPMC viscosity grades, namely K4M, E4M, K15 and K200M. Directly compressed tablets revealed an excellent uniformity in hardness, thickness and weight and nizatidine was evenly distributed within the matrix floating tablets. Buoyancy study revealed floating lag time as low as 18–38 s, and tablets remain buoyant for upto 24 h. However, the later depended upon viscosity grade of HPMC and that the higher the viscosity, the less was the total floating time. In vitro dissolution indicated viscosity dependent nizatidine release from the floating tablets. HPMC K4M and E4M based floating tablets released almost 100% drug in 12 h, whilst higher viscosity polymers such as K15 and K200M only released 81.88% and 75.81% drug, respectively. The drug release followed non-Fickian diffusion from tablets formulated with K4M, K15 and K200M, whilst super case II transport was observed with E4M based tablets. More interestingly, K4M and E4M polymers have similar viscosity yet exhibited different drug release mechanism. This was attributed to the difference in degree of substitution of methoxyl- and hydroxypropoxyl- groups on polymer backbone.

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Influence of polymer ratio and surfactants on controlled drug release from cellulosic microsponges

Cited by 48 publications

References 32 publications

Probing the effect of various lipids and polymer blends on clopidogrel encapsulated floating microcarriers

Probing the effect of various lipids and polymer blends on clopidogrel encapsulated floating microcarriers

Formulation and characterization of lornoxicam-loaded cellulosic-microsponge gel for possible applications in arthritis

Relevancy of Nizatidine Release from Floating Tablets with Viscosity of Various Cellulose Ethers

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