Carvedilol Solubility Enhancement by Inclusion Complexation and Solid Dispersion: Review

Abstract

Carvedilol is an effective nonselective alpha-1 and beta blocker discovered by Fritz Wiedemann [1]. It is an antihypertensive drug indicated for the treatment of mild to severe congestive heart failure (CHF), angina pectoris, cardiac arrhythmias and myocardial infarction [2]. Water solubility of Carvedilol is a fundamental property that affects the drug absorption after oral administration. Moreover, its dissolution and gastrointestinal permeability are the parameters that control its bioavailability [3]. The most frequent causes of low oral bioavailability is attributed to poor solubility and low permeability [4]. Carvedilol is categorized as class II drug with low solubility and reasonable membrane permeability. Cyclodextrins are cyclic (α-1,4)-linked oligosaccharides of α-D-glucopyranose, containing a relatively hydrophobic central cavity and hydrophilic outer surface [5]. Drug solubility enhancement using Cyclodextrin and

Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug for gastroretention

“…Structural formula of Carvedilol Mechanism of action: Carvedilol is a racemic mixture in which nonselective β-adrenoreceptor blocking activity is present in the S(-) enantiomer and α1-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol has no intrinsic sympathomimetic activity 19 .…”

“…To overcome problem of poor aqueous solubility of Carvedilol, various approaches have been investigated including physical and chemical modifications of the drug. 19 These mucoadhesive polymeric nanoparticles in the stomach will offer various advantages such as (i) Longer residence time of the dosage form on mucosal tissues in the stomach. This will improve absorption of the drug and increase the drug bioavailability.…”

Solubility Enhancement of Poor Water Soluble Drugs by Solid Dispersion: A Review

“…Several methods have been introduced to triumph over this problem. 1 , 2 Various methods to increase the solubility of drugs are available such as solid dispersion, self emulsifying drug delivery, Liquisolid techniques etc, in which drug in solution state or dissolved drug is adsorbed over insoluble carriers [3][4][5][6] Model list of Essential Medicines of the World Health Organization (WHO) has assigned BCS (Biopharmaceutics Classification System) classification on the basis of data available in the public domain. Out of 130 orally administered drugs on the WHO list, 61 could be classified with certainty.…”

Towards Rational Chemosensor Design through Improved Understanding of Experimental Parameter Variation and Tolerance in Cyclodextrin-Promoted Fluorescence Detection

“…Cyclodextrins are supramolecular hosts that are used widely for a variety of applications, including drug delivery [1][2][3], odor neutralization [4], supramolecular catalysis [5][6][7], and toxicant detection [8,9]. Their hydrophobic interiors allow them to form inclusion complexes with hydrophobic guests [10,11], while their hydrophilic exteriors impart aqueous solubility [12,13]. Previous work by our group has demonstrated the use of cyclodextrin host-guest complexes for toxicant detection applications through the promotion of cyclodextrin-based supramolecular complexes between a small molecule toxicant and a high quantum yield organic fluorophore [14].…”