Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs

Junyaprasert, Varaporn Buraphacheep; Morakul, Boontida

doi:10.1016/j.ajps.2014.08.005

Cited by 355 publications

(224 citation statements)

References 48 publications

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“…Another possible explanation for the increase in saturation solubility can be given by Kelvin equation which states that the dissolution pressure increases with increasing curvature, which means decreasing particle size. 14 The curvature is enormous when the particle size is in the nanometer range. The fold increase in the solubility of nanocrystal over pure drug is depicted in Table 4.…”

Section: H96 Approach For Aprepitant Nanosuspensionmentioning

confidence: 99%

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

S¹,

Deshpande²,

Attari³

et al. 2016

Adv Pharm Bull

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Section: H96 Approach For Aprepitant Nanosuspensionmentioning

confidence: 99%

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

S¹,

Deshpande²,

Attari³

et al. 2016

Adv Pharm Bull

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“…The latter approach involves size reduction of particles to nano range by using high-pressure homogenization (HPH) or milling techniques. 15 Of late, another newer technique that is, hot-melt extrusion with HPH is slowly gaining importance. 16 In the present study, the nanocrystals approach to improve the solubility of a poorly soluble drug aceclofenac (ACF) was attempted using wet milling method by utilizing Quality by Design (QbD) approach.…”

Section: Introductionmentioning

confidence: 99%

“…15 The positive sign of coefficients for the concentration of PVA and amount of ACF indicates that the particle size increases as the value of the variables increases. The effect of the parameters is clearly observed in the 3D plots shown in Figure 1A-F. As per the reports, an increase in the PVA concentration increases the particle size due to the increased viscosity of the dispersion medium, resulting in decreased attrition between balls and particles and also leading to greater amount of coating on the particle surface.…”

mentioning

confidence: 99%

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

Narayan¹,

Pednekar²,

Bhuyan³

et al. 2017

IJN

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The aim of the present work was to tackle the solubility issue of a biopharmaceutics classification system (BCS)-II drug, aceclofenac. Although a number of attempts to increase the aqueous solubility have been made, none of the methods were taken up for scale-up. Hence size reduction technique by a top-down approach using wet milling process was utilized to improve the solubility and, consequently, the dissolution velocity of aceclofenac. The quality of the final product was ensured by Quality by Design approach wherein the effects of critical material attributes and critical process parameters were assessed on the critical quality attributes (CQAs) of nanocrystals. Box–Behnken design was applied to evaluate these effects on critical quality attributes. The optimized nanocrystals had a particle size of 484.7±54.12 nm with a polydispersity index (PDI) of 0.108±0.009. The solid state characterization of the formulation revealed that the crystalline nature of the drug was slightly reduced after the milling process. With the reduced particle size, the solubility of the nanocrystals was found to increase in both water and 0.1 N HCl when compared with that of unmilled pure aceclofenac. These results were further supported by in vitro release studies of nanocrystals where an appreciable dissolution velocity with 100.07%±2.38% release was observed for aceclofenac nanocrystals compared with 47.66%±4.53% release for pure unmilled aceclofenac at the end of 2 h. The in vivo pharmacokinetic data generated showed a statistically significant increase in the C max for aceclofenac nanocrystals of 3.75±0.28 µg/mL (for pure unmilled aceclofenac C max was 1.96±0.17 µg/mL). The results obtained indicated that the developed nanocrystals of aceclofenac were successful in improving the solubility, thus the absorption and bioavailability of the drug. Hence, it may be a viable and cost-effective alternative to the current therapy.

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“…Several techniques have been explored to formulate co-crystals, such as melting extrusion [10], supercritical fluids [11], forming a slurry with ultrasound [12], micronize particles [13], solid grinding [14], spray drying [15], and solvent evaporation (SE) [16]. The SE method is widely used in pharmaceutical manufacturing [17].…”

Section: Introductionmentioning

confidence: 99%