Polymeric Excipients in the Technology of Floating Drug Delivery Systems

Blynskaya, E. V.; Tishkov, Sergey; Vinogradov, V. P.; Alekseev, K. V.; Marakhova, Anna I.; Vetcher, Alexandre A.

doi:10.3390/pharmaceutics14122779

Cited by 4 publications

(3 citation statements)

References 145 publications

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“…To overcome the low residence time of DDSs in the gastrointestinal tract (GIT), researchers have utilized floating DDSs (mainly suitable for delivery in the stomach [ 12 ]) and mucoadhesive DDSs. Mucoadhesive DDSs adhere to the intestinal mucous, prolonging their resident time and thereby improving systemic uptake [ 13 ]. For example, Rosso et al employed bioadhesive chitosan sponges to extend intestinal residence time to 6 h from the 3 h observed without chitosan [ 14 ].…”

Section: Introductionmentioning

confidence: 99%

Algae-Based Nanoparticles for Oral Drug Delivery Systems

Drori,

Patel,

Coopersmith

et al. 2024

Marine Drugs

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Drug administration by oral delivery is the preferred route, regardless of some remaining challenges, such as short resident time and toxicity issues. One strategy to overcome these barriers is utilizing mucoadhesive vectors that can increase intestinal resident time and systemic uptake. In this study, biomimetic nanoparticles (NPs) were produced from 14 types of edible algae and evaluated for usage as oral DDSs by measuring their size, surface charge, morphology, encapsulation efficiency, mucoadhesion force, and cellular uptake into Caco-2 cells. The NPs composed of algal materials (aNPs) exhibited a spherical morphology with a size range of 126–606 nm and a surface charge of −9 to −38 mV. The mucoadhesive forces tested ex vivo against mice, pigs, and sheep intestines revealed significant variation between algae and animal models. Notably, Arthospira platensis (i.e., Spirulina) NPs (126 ± 2 nm, −38 ± 3 mV) consistently exhibited the highest mucoadhesive forces (up to 3127 ± 272 µN/mm²). Moreover, a correlation was found between high mucoadhesive force and high cellular uptake into Caco-2 cells, further supporting the potential of aNPs by indicating their ability to facilitate drug absorption into the human intestinal epithelium. The results presented herein serve as a proof of concept for the possibility of aNPs as oral drug delivery vehicles.

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Section: Introductionmentioning

confidence: 99%

Algae-Based Nanoparticles for Oral Drug Delivery Systems

Drori,

Patel,

Coopersmith

et al. 2024

Marine Drugs

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“…[ 18 ], whereas formulating it as oil-entrapped beads not only improves solubility but also aids in achieving the sustained activity of the drug [ 19 , 20 , 21 ]. Sodium alginate is used as a polymer to localise and retain the drug in acidic environments; the polymer is selected due to its biocompatibility [ 22 , 23 ], biodegradability, mucoadhesive property [ 24 ], and nontoxicity [ 25 , 26 , 27 ].…”

Section: Introductionmentioning

confidence: 99%

Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

et al. 2023

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Background: Antihypertensive drug telmisartan (TEL) belongs to BCS class II, which is characterized by low water solubility and, consequently, low oral bioavailability. Gastroretentive systems may overcome the problems associated with low solubility of TEL and incomplete absorption by localizing the drug release in the stomach. The purpose of this study was to prepare TEL-loaded, oil-entrapped, floating alginate beads with the intent of enhancing the oral bioavailability of TEL for the treatment of hypertension. Methods: For the formulation and optimization of seventeen formulations of TEL-loaded oil-entrapped floating alginate beads, a central composite design was utilized. The concentration of sodium alginate (X1), the concentration of cross-linker (X2), and the concentration of sesame oil (X3) served as independent variables, whereas the entrapment efficiency (Y1), in vitro buoyancy (Y2), and drug release Q6h (Y3) served as dependent variables. Using the emulsion gelation method and calcium chloride as the cross-linking agent, different formulations of TEL alginate beads were produced. All formulations were evaluated for their entrapment efficiency percentage, in vitro buoyancy, and in vitro drug release. The optimal formulation of TEL alginate beads was prepared with and without oil and evaluated for entrapment efficiency percentage, in vitro buoyancy, swelling ratio, average size, and in vitro drug release. Using scanning electron microscopes, the surface morphology was determined. Using IR spectroscopy, the compatibility between the ingredients was determined. In vivo evaluation of the optimized formulation in comparison to the free TEL was done in hypertension-induced rats, and the systolic blood pressure and all pharmacokinetic parameters were measured. Results: The prepared beads exhibited a high entrapment efficiency percentage, in vitro buoyancy, and prolonged drug release. TEL was compatible with other ingredients, as approved by IR spectroscopy. The prepared TEL beads were spherical, as shown by the SEM. The relative bioavailability of TEL-loaded oil-entrapped beads was 222.52%, which was higher than that of the pure TEL suspension. The prepared TEL beads formulation exhibited a higher antihypertensive effect for a prolonged time compared to pure TEL suspension. Conclusions: It can be concluded that this innovative delivery method of TEL-loaded oil-entrapped beads is a promising tool for enhancing drug solubility and, thus, oral bioavailability and therapeutic efficacy, resulting in enhanced patient compliance. Furthermore, the in vivo study confirmed the formulation’s extended anti-hypertensive activity in animal models.

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“…Several formulation technologies, including microspheres, tablets, beads, films, and ring capsules, have this combination characteristic (Das et al, 2021;Pawar et al, 2011;Singh et al, 2011). In this case, excipients with certain characteristics are needed to combine the two systems (Blynskaya et al, 2022).…”

Section: Introductionmentioning

confidence: 99%

Chitosan as floating-mucoadhesive polymers in gastroretentive drug delivery

Ainurofiq,

Putri Febrina Sari,

Mardhiyah

et al. 2023

SEHS

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Oral drug delivery is limited by incomplete absorption in the digestive tract. The absorption of oral drugs in the stomach is affected by several factors, including gastric residence time, which causes the drug to be unable to be retained in the stomach for a long time, causing suboptimal drug absorption. One of the drug delivery systems that can prolong contact duration within the stomach is gastroretentive drug delivery system (GRDDS). GRDDS has various advantages, notably in improving the bioavailability of drugs. Several systems are involved in the GRDDS, including the floating and mucoadhesive systems. The floating system makes the drug float so it can be retained longer in the stomach. There are two mechanisms in the floating system: the effervescent and non-effervescent mechanisms. The mucoadhesive system works by adhering to the mucus or epithelial cells of the stomach. The mechanisms of mucoadhesive systems involves two stages: the contact and consolidation stages. The combination of the floating and mucoadhesive systems is aimed to improve the efficiency and effectiveness of a preparation for prolonged retention in the stomach. The choice of polymer is one of the crucial factors affecting this system. Chitosan is a natural polymer that has been evaluated for its potential in a gastroretentive floating beads delivery system. It has various advantageous properties, such as non-toxicity, biocompatibility, and biodegradability.

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Polymeric Excipients in the Technology of Floating Drug Delivery Systems

Cited by 4 publications

References 145 publications

Algae-Based Nanoparticles for Oral Drug Delivery Systems

Algae-Based Nanoparticles for Oral Drug Delivery Systems

Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

Chitosan as floating-mucoadhesive polymers in gastroretentive drug delivery

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