In Vitro and In Vivo Test Methods for the Evaluation of Gastroretentive Dosage Forms

Schneider, Felix; Koziolek, Mirko

doi:10.3390/pharmaceutics11080416

Cited by 50 publications

(34 citation statements)

References 148 publications

(295 reference statements)

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“…In Vivo studies were performed to assess the mucoadhesion property of prepared nanoparticles in Sprague Dawley rats [37]. The amount of sitagliptin adhered in the GIT membrane at various time intervals was determined after oral administration of prepared nanoparticles and compared with control (suspension of pure sitagliptin) ( Figure 12).…”

Section: Drug Retention In Gitmentioning

confidence: 99%

HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

et al. 2019

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Mucoadhesive nanoparticles represent a potential drug delivery strategy to enhance the therapeutic efficacy in oral therapy. This study assessed the prospective of developing HPMC- and PLGA-based nanoparticles using a nanospray drier as a mucoadhesive extended release drug delivery system for sitagliptin and evaluated their potential in an animal model. Nanoparticles were prepared using a Buchi® B-90 nanospray drier. Optimization of particle size was performed using response surface methodology by examining the influence of spray-drying process variables (inlet temperature, feed flow, and polymer concentration) on the particle size. The prepared nanoparticles were characterized for various physicochemical characteristics (yield, drug content, morphology, particle size, thermal, and crystallographic properties) and assessed for drug release, stability, and mucoadhesive efficacy by ex vivo and in vivo studies in rats. A linear model was suggested by the design of the experiments to be the best fit for the generated design and values. The yield was 77 ± 4%, and the drug content was 90.5 ± 3.5%. Prepared nanoparticles showed an average particle size of 448.8 nm, with a narrow particle size distribution, and were wrinkled. Thermal and crystallographic characteristics showed that the drug present in the nanoparticles is in amorphous dispersion. Nanoparticles exhibited a biphasic drug release with an initial rapid release (24.9 ± 2.7% at 30 min) and a prolonged release (98.9 ± 1.8% up to 12 h). The ex vivo mucoadhesive studies confirmed the adherence of nanoparticles in stomach mucosa for a long period. Histopathological assessment showed that the formulation is safe for oral drug delivery. Nanoparticles showed a significantly higher (p < 0.05) amount of sitagliptin retention in the GIT (gastrointestinal tract) as compared to control. The data observed in this study indicate that the prepared mucoadhesive nanoparticles can be an effective alternative delivery system for the oral therapy of sitagliptin.

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Section: Drug Retention In Gitmentioning

confidence: 99%

HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

et al. 2019

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“…During compression of the sample in the texture analysis, a small amount of water was pressed out from the samples immersed in the acidic media for 4 h. It can be explained by the poor wetting angle of BaSO 4 [34], as well. Incorporation of BaSO 4 into test formulations is often used to check gastric retention in vivo [35]. Samples were detected and identified easily in the in vivo test.…”

Section: Discussionmentioning

confidence: 99%

Process Optimization for the Continuous Production of a Gastroretentive Dosage Form Based on Melt Foaming

et al. 2021

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Several drugs have poor oral bioavailability due to low or incomplete absorption which is affected by various effects as pH, motility of GI, and enzyme activity. The gastroretentive drug delivery systems are able to deal with these problems by prolonging the gastric residence time, while increasing the therapeutic efficacy of drugs. Previously, we developed a novel technology to foam hot and molten dispersions on atmospheric pressure by a batch-type in-house apparatus. Our aim was to upgrade this technology by a new continuous lab-scale apparatus and confirm that our formulations are gastroretentive. At first, we designed and built the apparatus and continuous production was optimized using a Box–Behnken experimental design. Then, we formulated barium sulfate-loaded samples with the optimal production parameters, which was suitable for in vivo imaging analysis. In vitro study proved the low density, namely 507 mg/cm3, and the microCT record showed high porosity with 40 μm average size of bubbles in the molten suspension. The BaSO4-loaded samples showed hard structure at room temperature and during the wetting test, the complete wetting was detected after 120 min. During the in vivo study, the X-ray taken showed the retention of the formulation in the rat stomach after 2 h. We can conclude that with our device low-density floating formulations were prepared with prolonged gastric residence time. This study provides a promising platform for marketed active ingredients with low bioavailability.

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“…The prolonged residence of DFs in the stomach, known as gastric retention, has various therapeutic and biopharmaceutical properties. Improvement of local activity in the stomach, increased concentrations in the stomach, increased patient compliance due to dose reduction or improved bioavailability of some drugs with windows in the upper GIT [3].…”

Section: Gastroretentive Drug Delivery System (Grrds)mentioning

confidence: 99%

“…These systems Fig. 7, with a density of about 3 g/cm 3 , persist in the abdominal cavities and can prevent its gradual contraction. A density of 2.6-2.8 g/cm 3 serves as a threshold value after which such systems can be maintained in the lower abdomen.…”

Section: High-density Systemsmentioning

confidence: 99%

In Vitro in Vivo Studies on Floating Microspheres for Gastroretentive Drug Delivery System: A Review

Krishna¹,

Kumar

Rajat

2021

Asian J Pharm Clin Res

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The purpose of writing this review on gastroretentive drug delivery systems (GRDDS) was to compile the recent literature with a special focus on various gastroretentive approaches that have recently become leading methodologies in the field of site-specific orally administered controlled release drug delivery. One of the complex processes in the human body is gastric emptying, as it is highly variable, which makes the in vivo performance of the drug delivery systems uncertain. GRDDS has gained immense popularity in the field of oral drug delivery recently. It is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with the conventional oral delivery system. Conventional drug delivery systems may not overcome the issues imposed by the gastrointestinal tract (GIT) such as incomplete release of drugs, decrease in dose effectiveness, and frequent dose requirement. To overcome this variability, a controlled drug delivery system with a prolonged gastric residence time of >12 h in the stomach can be of great practical importance for drugs with an absorption window in the upper small intestine. GRDFs enable prolonged and continuous release of the drug to the upper part of the GIT and thus significantly extend the duration of drug release and improve the bioavailability of drugs that have a narrow therapeutic window; by this way, they prolong dosing interval and increase compliance.

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In Vitro and In Vivo Test Methods for the Evaluation of Gastroretentive Dosage Forms

Cited by 50 publications

References 148 publications

HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

Process Optimization for the Continuous Production of a Gastroretentive Dosage Form Based on Melt Foaming

In Vitro in Vivo Studies on Floating Microspheres for Gastroretentive Drug Delivery System: A Review

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