Gellan gum based gastroretentive tablets for bioavailability enhancement of cilnidipine in human volunteers

Karemore, Megha N.; Bali, Nikhil

doi:10.1016/j.ijbiomac.2021.01.199

Cited by 17 publications

(4 citation statements)

References 65 publications

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“…Finally, the tablets demonstrated promising gastric retention and drug release results in human volunteers, indicated by a prolonged half-life and reduced elimination rate of cilnidipine, compared to conventional tablets. These findings further demonstrated the potential of the cilnidipine gastroretentive tablet application [202].…”

Section: Floating and Mucoadhesive Systemssupporting

confidence: 53%

“…Karemore et al focused on the development of a cilnidipine effervescent floating gastroretentive tablet formulation that contained gellan gum as the bioadhesive polymer, as well as HPMC K4M and sodium bicarbonate as excipients that can aid in floatation and controlled drug release [202]. The amounts of these three components had a statistically significant effect on the floating lag time, total floating time, mucoadhesion and in vitro drug release properties of the tablets.…”

Section: Floating and Mucoadhesive Systemsmentioning

confidence: 99%

“…An increase in the amount of these components significantly reduced the floating lag time and prolonged the floatation of tablets. This was due to the increased swelling of the polymers, alongside the entrapment of CO 2 bubbles generated from the reaction of sodium bicarbonate with hydrochloric acid [202]. Furthermore, sodium bicarbonate acted as a source of sodium ions which promoted the in situ gelation of GG through the formation of a cross-linked, three-dimensional network [203][204][205][206].…”

Section: Floating and Mucoadhesive Systemsmentioning

confidence: 99%

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Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

2021

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There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologies have the potential to achieve retention of the dosage form in the upper gastrointestinal tract (GIT) that can be sufficient to ensure complete solubilisation of the drugs in the stomach fluids, followed by subsequent absorption in the stomach or proximal small intestine. This can be beneficial for drugs that have an “absorption window” or are absorbed to a different extent in various segments of the GIT. Therefore, gastroretentive technologies in tandem with controlled-release strategies could enhance both the therapeutic efficacy of many drugs and improve patient compliance through a reduction in dosing frequency. The paper reviews different gastroretentive drug delivery technologies and controlled-release strategies that can be combined and summarises examples of formulations currently in clinical development and commercially available gastroretentive controlled-release products. The different parameters that need to be considered and monitored during formulation development for these pharmaceutical applications are highlighted.

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Section: Floating and Mucoadhesive Systemssupporting

confidence: 53%

Section: Floating and Mucoadhesive Systemsmentioning

confidence: 99%

Section: Floating and Mucoadhesive Systemsmentioning

confidence: 99%

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Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

2021

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“…This approach allows for extending the formulation residence time at the administration site and therefore improves the bioavailability of the active ingredient. Mucoadhesive formulations are usually administered to oral [ 18 ], vaginal [ 19 ] and nasal [ 20 , 21 ] mucosa but there are also examples of particulate formulations [ 22 ] or tablets [ 23 ] administered orally and adhering to gastric mucosa. However, in the case of formulations aiming at the mucoadhesive effect, usually chemically modified gums with thiol groups introduced to the structure are obtained and investigated [ 24 , 25 , 26 , 27 ].…”

Section: Natural Gumsmentioning

confidence: 99%

Natural Gums in Drug-Loaded Micro- and Nanogels

et al. 2023

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Gums are polysaccharide compounds obtained from natural sources, such as plants, algae and bacteria. Because of their excellent biocompatibility and biodegradability, as well as their ability to swell and their sensitivity to degradation by the colon microbiome, they are regarded as interesting potential drug carriers. In order to obtain properties differing from the original compounds, blends with other polymers and chemical modifications are usually applied. Gums and gum-derived compounds can be applied in the form of macroscopic hydrogels or can be formulated into particulate systems that can deliver the drugs via different administration routes. In this review, we present and summarize the most recent studies regarding micro- and nanoparticles obtained with the use of gums extensively investigated in pharmaceutical technology, their derivatives and blends with other polymers. This review focuses on the most important aspects of micro- and nanoparticulate systems formulation and their application as drug carriers, as well as the challenges related to these formulations.

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Development and in Vitro/In Vivo Evaluation of Itopride Hydrochloride Expanding Tablets

et al. 2023

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Purpose Gastroretentive drug delivery systems (GRDDS) have attracted interest for enhancement of absorption and bioavailability of some drugs. Itopride hydrochloride (ITOP) is a drug used for treatment of gastroesophageal reflux and other gastric motility disorders, but is characterized by narrow absorption window and short in vivo half-life. Therefore, it is expected that its formulation in expanding gastroretentive tablets would increase its gastric residence, thus leading to decreased frequency of administration and increased patient compliance. Methods The direct compression method was used for formulation of tablets. Four different hydrophilic polymers (xanthan gum, sodium alginate, gellan gum, pectin) were screened separately with Avicel 102 and PVP k30 as excipients. The effect of different factors (polymer type and amount, and excipient amount) on the tablet properties such as hardness, friability, thickness, diameter, weight variation, swelling, and in vitro drug dissolution was studied. In addition, swelling test, accelerated stability test, and in vivo study were performed on the optimized formulation. Results Tablets prepared using xanthan gum exhibited favorable properties compared to tablets prepared using the other gums, however increasing the polymer amount led to increased tablet friability. The selected formulation exhibited obvious expansion reaching 17.45 mm and lasting for 24 h, coupled with a sustained release behavior. X-ray scans in human volunteers suggested the residence of the tablet in the stomach for a period of 6 h in fed state. Conclusion Successful preparation of directly compressible ITOP expanding tablets was achieved in this study, which is expected to result in better therapeutic outcome in gastroesophageal reflux.

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Gellan gum based gastroretentive tablets for bioavailability enhancement of cilnidipine in human volunteers

Cited by 17 publications

References 65 publications

Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

Natural Gums in Drug-Loaded Micro- and Nanogels

Development and in Vitro/In Vivo Evaluation of Itopride Hydrochloride Expanding Tablets

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