Solubility Enhancement Techniques for Poorly Water-Soluble Drugs

Deshmukh, Amol S.; Tiwari, Kundan J; Mahajan, Vijay R.

doi:10.37285/ijpsn.2017.10.3.1

Cited by 19 publications

(14 citation statements)

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“…Mono nuclear phagocytic system must absorb the drug to allow regional specific delivery. 52 This may be used to target macrophages with anti microbacterial, leishmanial drugs if the infectious pathogen persists intracellularly.…”

Section: Drug Targetingmentioning

confidence: 99%

Nanosuspension as Promising and Potential Drug Delivery: A Review

Chinthaginjala¹,

Ahad²,

Reddy³

et al. 2022

Int J Life Sci Pharm Res

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In the last decade, nanosuspensions have gained considerable interest as a method for formulating poorly soluble drugs. Because of their cost-effectiveness and technological simplicity compared to liposomes and other colloidal drug carriers, nanoscale systems have recently received a lot of attention as a way of solving problems of solubility. Nanosuspensions are biphasic systems comprising of pure drug particles dispersed in an aqueous vehicle, stabilized by surface active agents. Fabrication of nanosuspension is simple and more advantageous than other approaches. Nanosuspension is a very finely single solid drug particle in an aqueous vessel, stabilized by surfactants for either oral or topical use or for parenteral and pulmonary administration, it can also be used for targeted drug delivery when incorporated in the ocular inserts and mucoadhesive hydrogels, with reduced particle size resulting in increased dissolution rate. This article covers the preparation of nanosuspension by bottom up technology, top down technology, melt emulsification, emulsification- solvent evaporation and supercritical fluid with their advantages and disadvantages, aspects of structure, classification and their drug delivery applications. Nanosuspension can be processed for the drugs which are of hydrophobic in nature quite easily employing stability enhancers, solvents that are of organic and additional ingredients including buffering agents, salts, PEG, osmotic agents and anti-freeze compounds.

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Section: Drug Targetingmentioning

confidence: 99%

Nanosuspension as Promising and Potential Drug Delivery: A Review

Chinthaginjala¹,

Ahad²,

Reddy³

et al. 2022

Int J Life Sci Pharm Res

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“…In pharmaceutical cocrystallization, solubility is a particularly important thermodynamic property. From a biological standpoint, solubility determines the concentration of the API in systemic circulation so it must be fine-tuned for achieving the required pharmacological response . From an engineering perspective, solubility curves are necessary for any crystallization process design and development. , Thus, several studies have been devoted to improving API solubility via cocrystallization with a coformer (CF) as well as finding the region in the phase diagram that favors cocrystal formation. − For instance, Darwish et al have successfully prepared a new 1:1 theophylline–aspirin cocrystal and then constructed the ternary phase diagram (TPD) to identify stable regions for cocrystal formation …”

Section: Introductionmentioning

confidence: 99%

Shortcut Method for the Prediction of the Cocrystal Solubility Line

Rapeenun

Rarey

Flood

2021

Crystal Growth & Design

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Knowledge of the solubility of a cocrystal in terms of solvent, temperature, and the liquid-phase concentrations of the active pharmaceutical ingredient and coformer is necessary for the pharmaceutical industry to produce pharmaceuticals with improved physicochemical properties. Here, we propose a simple and convenient shortcut calculation to predict the solubility curve of cocrystals using simple thermodynamic equations, considering the liquid-phase activity coefficient of the two species in the cocrystal, which does not require any fitting nor experimental solubility data of the cocrystal. Ibuprofen–nicotinamide and carbamazepine–nicotinamide cocrystals in ethanol were used to study the effect of temperature variation, while indomethacin–saccharin and carbamazepine–nicotinamide cocrystals were used to study the effect of solvents. Our prediction shows good results in both scenarios, which were supported by the absolute average deviation and the percent absolute relative deviation (% ARD) from the experimental data. Carbamazepine–nicotinamide in ethanol shows the best outcome with the lowest % ARD (9.0, 24.6, and 8.6% at 288.15, 298.15, and 308.15 K, respectively). Furthermore, we also illustrate the importance of the activity coefficient and any phase transition of the pure species in the calculation to achieve the most accurate result.

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“…Currently, amorphization is considered one of the best methods to deliver insoluble drugs, especially those belonging to the II and IV BCS groups [ 23 , 24 ]. Numerous cases of increased solubility of API after obtaining amorphous dispersion have been described in the literature.…”

Section: Introductionmentioning

confidence: 99%

Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as a Way to Enhance Dissolution Rate and Permeability

Wiergowska¹,

Ludowicz

Wdowiak

et al. 2021

Pharmaceuticals

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To improve physicochemical properties of vardenafil hydrochloride (VAR), its amorphous form and combinations with excipients—hydroxypropyl methylcellulose (HPMC) and β-cyclodextrin (β-CD)—were prepared. The impact of the modification on physicochemical properties was estimated by comparing amorphous mixtures of VAR to their crystalline form. The amorphous form of VAR was obtained as a result of the freeze-drying process. Confirmation of the identity of the amorphous dispersion of VAR was obtained through the use of comprehensive analysis techniques—X-ray powder diffraction (PXRD) and differential scanning calorimetry (DSC), supported by FT-IR (Fourier-transform infrared spectroscopy) coupled with density functional theory (DFT) calculations. The amorphous mixtures of VAR increased its apparent solubility compared to the crystalline form. Moreover, a nearly 1.3-fold increase of amorphous VAR permeability through membranes simulating gastrointestinal epithelium as a consequence of the changes of apparent solubility (Papp crystalline VAR = 6.83 × 10−6 cm/s vs. Papp amorphous VAR = 8.75 × 10−6 cm/s) was observed, especially for its combinations with β-CD in the ratio of 1:5—more than 1.5-fold increase (Papp amorphous VAR = 8.75 × 10−6 cm/s vs. Papp amorphous VAR:β-CD 1:5 = 13.43 × 10−6 cm/s). The stability of the amorphous VAR was confirmed for 7 months. The HPMC and β-CD are effective modifiers of its apparent solubility and permeation through membranes simulating gastrointestinal epithelium, suggesting a possibility of a stronger pharmacological effect.

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Solubility Enhancement Techniques for Poorly Water-Soluble Drugs

Cited by 19 publications

References 0 publications

Nanosuspension as Promising and Potential Drug Delivery: A Review

Nanosuspension as Promising and Potential Drug Delivery: A Review

Shortcut Method for the Prediction of the Cocrystal Solubility Line

Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as a Way to Enhance Dissolution Rate and Permeability

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