Extensive Diminution of Particle Size and Amorphization of a Crystalline Drug Attained by Eminent Technology of Solid Dispersion: A Comparative Study

Singh, Gurbax; Sharma, Shailesh; Gupta, Gagan

doi:10.1208/s12249-016-0647-3

Cited by 15 publications

(17 citation statements)

References 24 publications

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“…In our experiment, the crystallinity of HAP produced after aging for two days in the TEA+ET group was better, which might have been due to the fact that the Ca(OH) 2 template was a smaller and more dispersed particle. The smaller and more dispersed particles increased the specific surface area and thereby increased the surface free energy, resulting in higher solubility and dissolution [34]. At the same time, according to the description of the Ostwald-Freundlich equation, a smaller particle size not only increases the specific surface area but also increases the saturated solubility, which further improves the dissolution rate [35].…”

Section: Causes Of Structural Of Micro/nano-sized Hapmentioning

confidence: 99%

Improvement of Drug-Loading Properties of Hydroxyapatite Particles Using Triethylamine as a Capping Agent: A Novel Approach

Wen

Lin

et al. 2021

Crystals

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Particles that modify delivery characteristics are a focus of drug-loading research. Hydroxyapatite particles (HAPs) have excellent biocompatibility, shape controllability, and high adsorption, making them a potential candidate for drug-delivery carriers. However, there are still some defects in the current methods used to prepare HAPs. In order to avoid agglomeration and improve the drug-loading properties of HAPs, the present study provides a novel triethylamine (TEA)-capped coprecipitation template method to prepare HAPs at room temperature. In addition, pure water and anhydrous ethanol were used as solvents to investigate the capping effect of the small-molecule capping agent TEA during the synthesis of HAPs. The results showed that the HAPs prepared in the TEA ethanol system had a smaller particle size (150–250 nm), better dispersion and higher crystallinity. The results were significantly different from those of the conventional preparation methods without TEA. However, the hydroxyapatite crystal would agglomerate to a certain extent after being stored for a period of time, forming micro/nano-sized agglomerates of nanocrystals. FITR analysis and SEM observation showed that the capping effect of TEA promoted the formation of a smaller template and dispersed HAPs were quickly formed by dissolution and reprecipitation processes. The drug-loading experiments showed that the HAPs prepared in the TEA ethanol system had high drug-loading capacity (239.8 ± 13.4 mg·g−1) as well as an improved drug-release profile demonstrated in the drug-release experiment. The larger specific surface area associated with the smaller particle size was beneficial to the adsorption of drugs. After drying at 60 °C, TEA was evaporated from the HAPs which agglomerated into larger micron particles with more drug encapsulated. Thus, the effect of a sustained release was achieved. In the present research, a novel approach was developed by using triethylamine as the capping agent to prepare micro/nano-sized agglomerates of HAP nanocrystals with improved drug loading, which is predicted to have potential application in drug delivery.

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Section: Causes Of Structural Of Micro/nano-sized Hapmentioning

confidence: 99%

Improvement of Drug-Loading Properties of Hydroxyapatite Particles Using Triethylamine as a Capping Agent: A Novel Approach

Wen

Lin

et al. 2021

Crystals

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“…Recently, Singh et al in their study proved the effectiveness of using natural polymers for enhancing the solubility of drug as compared to synthetic polymers. The results were better analysed by determining the particle size of prepared dispersions by using particle size analyser and which were found to be in nanometric size and possessed utmost solubility upon usage of locust bean gum as a carrier [45] .…”

Section: Novel Technologies Associated With Solid Dispersionsmentioning

confidence: 99%

Enhancement of the Solubility of Poorly Water Soluble Drugs through Solid Dispersion: A Comprehensive Review

Singh¹,

Kaur²,

Gupta³

et al. 2017

pharmaceutical-sciences

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Absorption of a drug through the oral route involves its dissolution from the formulation into gastric and/ or intestinal fluids followed by its permeation through gastrointestinal cell membranes and finally into the systemic circulation. Oral solid dosage forms are one of the most commonly used formulation types having multiple benefits over other formulations/routes. However, the challenge for a pharmaceutical scientist lies in the fact that dissolution of a drug from an oral solid formulation (a key factor in drug absorption) is dependent on the aqueous solubility of the drug. Therefore, a drug with poor aqueous solubility would exhibit dissolution rate limited absorption and similarly a drug possessing poor membrane permeability undergo permeation rate limited absorption. A drug is highly soluble when highest dose of drug is soluble in ≤250 ml of water over a pH range of 1 to 7.5 and a drug is highly permeable when extent of absorption in humans is to be ≥90% of an administered dose [1] . It has been investigated that most of new chemical entities currently being discovered and intended to be used as a solid dosage form should produce an efficient and reproducible plasma concentration after oral administration. However, most of them tend to have poor water solubility, which limits the therapeutic efficacy of that drug. Moreover, poor solubility results in increased dose and frequent administration leading to higher incidences of side-effects [2][3][4][5][6] . Hence, pharmaceutical research has emphasised on elevating the oral bioavailability of poorly water-soluble drugs by improving their solubility, dissolution rate and membrane permeability. Solubility is an important determinant in drug liberation and hence drug absorption, which plays a key role in oral bioavailability of formulations. The dissolution rate of a drug directly depends upon its solubility. Most of the new drugs have poor water solubility; thereby pose a difficulty in formulating into drug delivery systems. Therefore, solubility enhancement of poorly water soluble drugs is one of the necessary preformulation steps in the pharmaceutical product development research. Solid dispersion is a unique and promising approach for enhancing the dissolution characteristics and oral bioavailability of poorly water-soluble drugs. The present review highlights portrayal of solid dispersions, its types including eutectic mixtures and solid solutions, method of preparation and also the useful carriers for the preparation of solid dispersions. Furthermore, the wide research conducted hitherto on solid dispersions for enhancing solubility of different efficacious drugs, challenges encountered in the development of solid dispersions and recent advancements to overcome its pitfalls have also been elaborated.

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“…With the development of high–throughput screening technology, many new chemical drugs have been developed [1,2,3]. It has been reported that more than 40% of new active substances cannot be used clinically because of their poor water solubility, resulting in low oral bioavailability and problems with oral absorption [4,5,6,7,8]. Therefore, in order to transform more insoluble candidate compounds into new therapeutic drugs and maximize their efficacy, enhancing the solubility and bioavailability of these drugs is an important scientific problem that urgently needs to be solved.…”

Section: Introductionmentioning

confidence: 99%

“…Solid dispersion technology is a promising strategy to improve the oral bioavailability of insoluble drugs [6,7]. Inorganic porous materials including Aerosil, Syslia and Parteck have been extensively applied as drug carriers for solid dispersions [8].…”

Section: Introductionmentioning

confidence: 99%

A Comparative Study of the Use of Mesoporous Carbon and Mesoporous Silica as Drug Carriers for Oral Delivery of the Water-Insoluble Drug Carvedilol

et al. 2019

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Mesoporous carriers have been extensively applied to improve the dissolution velocity and bioavailability of insoluble drugs. The goal of this work was to compare the drug-loading efficiency (LE) and drug-dissolution properties of mesoporous silica nanoparticles (MSN) and mesoporous carbon nanoparticles (MCN) as drug vectors oral delivery of water-insoluble drugs. For this purpose, MSN and MCN with similar particle size, surface area, and mesoporous diameter were prepared to precisely evaluate the effects of different textures on the drug-loading and dissolution behavior of insoluble drugs. Carvedilol (CAR), a Bio-pharmaceutic Classification System (BCS) class II drug, was loaded in the MSN and MCN by the solvent adsorption method and solvent evaporation method with different carrier–drug ratios. The carboxylated MCN (MCN–COOH) had a higher LE for CAR than MSN for both the two loading methods due to the strong adsorption effect and π–π stacking force with CAR. In vitro drug dissolution study showed that both MSN and MCN-COOH could improve the dissolution rate of CAR compared with the micronized CAR. In comparison to MSN, MCN-COOH displayed a slightly slower dissolution profile, which may be ascribed to the strong interaction between MCN-COOH and CAR. Observation of cell cytotoxicity and gastrointestinal mucosa irritation demonstrated the good biocompatibility of both MSN and MCN–COOH. The present study encourages further research of different carriers to determine their potential application in oral administration.

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Extensive Diminution of Particle Size and Amorphization of a Crystalline Drug Attained by Eminent Technology of Solid Dispersion: A Comparative Study

Cited by 15 publications

References 24 publications

Improvement of Drug-Loading Properties of Hydroxyapatite Particles Using Triethylamine as a Capping Agent: A Novel Approach

Improvement of Drug-Loading Properties of Hydroxyapatite Particles Using Triethylamine as a Capping Agent: A Novel Approach

Enhancement of the Solubility of Poorly Water Soluble Drugs through Solid Dispersion: A Comprehensive Review

A Comparative Study of the Use of Mesoporous Carbon and Mesoporous Silica as Drug Carriers for Oral Delivery of the Water-Insoluble Drug Carvedilol

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