Electrospun orally disintegrating film formulation of telmisartan

Birer, Mehmet; Acartürk, Füsun

doi:10.1080/10837450.2021.1916031

Cited by 14 publications

(4 citation statements)

References 58 publications

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“…Electrospun nanofibers (Figure 2) are polymeric-based structures that possess diverse customary properties that make them interesting to be used as drug carriers [13], these characteristics include biocompatibility [14,15], biodegradability [16,17], high surface area [18,19], adequate mechanical properties [20,21], highly customizable fiber diameter and structure [22,23], excellent porosity connectivity [24,25], ease of handling [26,27], functionalization [28,29], and the ability to encapsulation of a diversity of bioactive molecules [30,31].…”

Section: Electrospun Nanofibersmentioning

confidence: 99%

Novel Drug Carries: Properties and Applications

Villarreal-Gómez¹,

Pérez-González²

2022

Drug Carriers

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Conventional drug administration has several issues and challenges such as full doses absorption and efficient targeting, some generate undesirable secondary effects and promote damage to organs and tissues such as the liver and kidneys, and others trigger inflammation and immune responses. Hence, drug carriers help to promote drug absorption, enhance targeting, avoid or decrease secondary effects, possess the ability to camouflage drugs from immune cells and proteins, and permit controlled release to provide prolonged drug delivery to maintain its blood concentration within therapeutic limits. Drug carriers have gained importance thanks to their various properties such as biocompatibility, biodegradability, mechanical properties, and high surface area, among others. Drug carriers are getting crucial to avoid or diminish secondary effects and improve the targeting of the administered drugs incrementing their effectiveness. Hence, this book chapter aims to introduce some drug carriers (electrospun nanofibers, aptamers, micelles, and liposomes), describing the properties and polymers used. It is observed that fast dissolving administration is the most recommended strategy for the use of drug carriers, where more evident therapeutics benefits can be appreciated.

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Section: Electrospun Nanofibersmentioning

confidence: 99%

Novel Drug Carries: Properties and Applications

Villarreal-Gómez¹,

Pérez-González²

2022

Drug Carriers

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“…Several techniques were used to enhance the drug solubility after oral administration and, hence, enhance their bioavailability [ 4 ]. These strategies include amorphous solid dispersions using synthetic polymers [ 5 ], the co-crystal technique [ 6 ], electrospinning [ 7 ], and floating beads [ 8 ]. Low-density floating beads have sufficient buoyancy to float over gastric contents and remain in the stomach for an extended period of time.…”

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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“…Tort and Acartürk (2016) prepared a nanofibrous ODF with HPMC, PEO, and sodium alginate with the addition of glutamine. The highest degree of elongation was achieved by Birer and Acartürk (2021) for nanofibrous films containing telmisartan and l-Arginine using a PVP matrix. The results revealed that the films produced via electrospinning had a higher Young's modulus E and exhibited a deterioration in their mechanical properties after 1 month.…”

Section: Introductionmentioning

confidence: 99%

Electrospun HPMC/PEO-blend orodispersible films: how slight batch differences affect the crucial mechanical properties

et al. 2023

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Orodispersible films comprise a promising dosage form with a wide range of advantages compared to conventional formulations. The electrospinning process can significantly enhance the relevant characteristics of orodispersible films, e.g., the dissolution rate and the ease of administration. This study involved the use of two types of hydroxypropyl methylcelluloses of low molecular weight obtained from three different manufacturers as the matrix. The SEM, FTIR, RAMAN, and DSC analyses revealed comparable values for all the fabricated materials. However, the mechanical properties of the fibers differed significantly, with electrospun Methocel E5/PEO proving to be particularly brittle. This is probably caused by the different arrangements of substituted methoxy- and hydroxypropyl groups of studied HPMCs. It is hoped that this paper will serve as an example of the extent to which slight differences between HPMC powder batches can dramatically alter the key properties of electrospun orodispersible films.

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Electrospun orally disintegrating film formulation of telmisartan

Cited by 14 publications

References 58 publications

Novel Drug Carries: Properties and Applications

Novel Drug Carries: Properties and Applications

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

Electrospun HPMC/PEO-blend orodispersible films: how slight batch differences affect the crucial mechanical properties

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