A Review on Solubility Enhancement of Carvedilol—a BCS Class II Drug

Fernandes, Gasper; Kumar, Lalit; Sharma, Kartik; Tunge, Rupa; Rathnanand, Mahalaxmi

doi:10.1007/s12247-018-9319-z

Cited by 39 publications

(22 citation statements)

References 35 publications

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“…Although carvedilol is well accepted in clinics, it undergoes first-pass metabolism and has low oral bioavailability (about 25% to 35%) [ 5 ]. The low oral bioavailability of carvedilol is possibly because of its low dissolution capability (ranked in the class II category of biopharmaceutical classification system), and its profound pre-systemic metabolism [ 6 , 7 ]. Therefore, there is a need to develop an alternative method for carvedilol delivery, such as transdermal delivery.…”

Section: Introductionmentioning

confidence: 99%

Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect

et al. 2021

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Background Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally. Ethosomes-mediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. The central composite design could be used as a tool to optimize ethosomal formulation. Thus, this study aims to optimize carvedilol-loaded ethosomes using central composite design, followed by incorporation of synthesized ethosomes into hydrogels for transdermal delivery of carvedilol. Results The optimized carvedilol-loaded ethosomes were spherical in shape. The optimized ethosomes had mean particle size of 130 ± 1.72 nm, entrapment efficiency of 99.12 ± 2.96%, cumulative drug release of 97.89 ± 3.7%, zeta potential of − 31 ± 1.8 mV, and polydispersity index of 0.230 ± 0.03. The in-vitro drug release showed sustained release of carvedilol from ethosomes and ethosomal hydrogel. Compared to free carvedilol-loaded hydrogel, the ethosomal gel showed increased penetration of carvedilol through the skin. Moreover, ethosomal hydrogels showed a gradual reduction in blood pressure for 24 h in rats. Conclusions Taken together, central composite design can be used for successful optimization of carvedilol-loaded ethosomes formulation, which can serve as the promising transdermal delivery system for carvedilol. Moreover the carvedilol-loaded ethosomal gel can extend the anti-hypertensive effect of carvedilol for a longer time, as compared to free carvedilol, suggesting its therapeutic potential in future clinics.

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Section: Introductionmentioning

confidence: 99%

Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect

et al. 2021

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“…Several techniques were being used to overcome this challenge; however, in the last decade, pharmaceutical multicomponent systems have gained increasing interest, including pharmaceutical co-crystals, salts, and more recently, CAMs [15]. Fernandes et al [16] emphasized the potential of co-crystals and CAMs in general and particularly for solubility enhancement of neutral molecules such as carvedilol. Various techniques are available for preparing pharmaceutical co-crystals, salts, and CAMs, some of which are solvent-based, whereas the others are solvent-free.…”

Section: Hme In Pharmaceutical Multicomponent Systemsmentioning

confidence: 99%

An update on the contribution of hot-melt extrusion technology to novel drug delivery in the twenty-first century: part II

Sarabu

Bandari

Kallakunta

et al. 2019

Expert Opinion on Drug Delivery

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Introduction: Interest in hot melt extrusion (HME) technology for novel applications is growing day by day, which is evident from several hundred publications within the last five years. HME is a cost-effective, solvent free, "green" technology utilized for various formulations with low investment costs compared to conventional technologies. HME has also earned the attention of the pharmaceutical industry by the transformation of this technology for application in continuous manufacturing.Areas covered: Part II of the review focuses on various novel opportunities or innovations of HME such as multiple component systems (co-crystals, co-amorphous systems and salts), twinscrew granulation, semi-solids, co-extrusion, abuse deterrent formulations, solid self-emulsifying drug delivery systems, chronotherapeutic drug delivery systems and miscellaneous applications.Expert opinion: HME is being investigated as an alternative technology for preparation of multi-component systems such as co-crystals and co-amorphous techniques. Twin-screw granulation has gained increased interest in preparation of granules via twin-screw melt granulation or twin-screw dry granulation. This novel application of the HME process provides a promising alternate approach in the formulation of granules and solid dosage forms. However, this technology may need to be further investigated for scalability aspects of these novel applications for industrial production.

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“…64 Co-crystallization approach for poorly soluble drugs like Carvedilol shown better bioavailability, solubility and dissolution in comparison to other strategies. 19 A NMR crystallographic study on niclosamide co-crystals, reported the improvement of equilibrium solubility of 1:1 niclosamide -thiazole cocrystals 2.8 folds to that of pristine niclosamide. 65…”

Section: Solubilitymentioning

confidence: 99%

“…12,13 Many of co-crystal strategies like solvent change techniques, 14 Solution co-crystallization, 15 thermal methods, 16 ultrasound assisted, 17 grinding methods 18 have been emerged. Previously, many of the case studies and reviews conducted in co-crystals reported, superiority of co-crystallization technology in comparison to other strategies, 19 improvements in manufacturing of drug dosage forms, 20 enhancements in drug properties by bottom-up approach, 21 pharmaceutical co-crystallization techniques, 22 translational development challenges, 23 impact of co-crystals on drug pharmacokinetics, 24 Co-crystallization of neutraceuticals, 25 Vibrational spectroscopic investigations on co-crystallization. 26 Improvement of physicochemical properties of co-crystallization have been well explored.…”

Section: Introductionmentioning

confidence: 99%

Insight into Concept and Progress on Pharmaceutical Co-Crystals: An overview

Vemuri¹,

Srinivas²

2019

IJPER

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Pharmaceutical co-crystals have conferred significant recognition in recent past as a new solid form by virtue their capability to modulate physicochemical properties of Active Pharmaceutical Ingredient (API). Nevertheless, pharmaceutical progress of cocrystals could be provocation, the requirement for high-throughput screening methods and the techniques capable of co-crystal production in industrial scale still hamper the co-crystal used by industries. In this review, well ordered overview of pharmaceutical co-crystal is provided, with focus on role of supramolecular chemistry, co-crystal design strategies, preparation methods, physicochemical property studies, mechanism of solubility enhancement, evaluation techniques. In the present commentary, the impact of choosing appropriate process design and formulation on translational challenges has been discussed. Eventually, a short outline of applications and marketed drug products of pharmaceutical co-crystal drug substance is also described.

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A Review on Solubility Enhancement of Carvedilol—a BCS Class II Drug

Cited by 39 publications

References 35 publications

Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect

Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect

An update on the contribution of hot-melt extrusion technology to novel drug delivery in the twenty-first century: part II

Insight into Concept and Progress on Pharmaceutical Co-Crystals: An overview

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