Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

Chokshi, Rina; Zia, Hossein; Sandhu, Harpreet; Shah, Navnit; Malick, Waseem

doi:10.1080/10717540600640278

Cited by 118 publications

(57 citation statements)

References 9 publications

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“…These drugloaded nanoparticles prepared by solid dispersion method have always small size and high DL compared with other methods as reported by recent articles (Chokshi et al, 2007). The obtained GEF-NPs were mono-dispersed (PDI < 0.22), smaller than 24 nm and could be well redissolve in water to meet the requirement of intravenous injection.…”

Section: Discussionmentioning

confidence: 75%

In vitro and in vivo antitumor effect of gefitinib nanoparticles on human lung cancer

Chen

Zhang

et al. 2017

Drug Delivery

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Gefitinib (GEF) is the first epidermal growth factor receptor (EGFR)-targeting agent launched as an anticancer drug. It is an accepted opinion that modifying GEF strong hydrophobicity and poor bioavailability would not only enhance its antitumor effects, but also reduce its side effects. In this study, GEF-loadedpoly(e-caprolactone)-poly(ethyleneglycol)-poly(e-caprolactone) (PCEC) -bearing nanoparticles (GEF-NPs) were prepared by a solid dispersion method and characterized. The particle sizes increased with the increase in GEF/PCEC mass ratio in feed. GEF-NPs (10%) were mono-dispersed, smaller than 24 nm, zeta potential was approximately À18 mV, percentage encapsulation and loading, were more than 9% and 92%, respectively, and drug was slowly released but without a biphasic pattern. Microscopy studies of the optimized formulation confirmed that the prepared nanoparticles are spherical in nature. Cytotoxicity results indicated that cell growth inhibition induced by free GEF and GEF-NPs were dose and time dependent. Compared with free GEF, GEF-NPs enhanced antitumor effects, reduced side effects and significantly prolonged survival time in vivo. CD31, ki-67 and EGFR expression were significantly lower in the GEF-NPs group compared with other groups (p< .05). These findings demonstrated that GEF-NPs have the potential to attain superior outcomes and to overcome complications such as organs toxicity, therapeutic resistance and disease relapse. ARTICLE HISTORY

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Section: Discussionmentioning

confidence: 75%

In vitro and in vivo antitumor effect of gefitinib nanoparticles on human lung cancer

Chen

Zhang

et al. 2017

Drug Delivery

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“…[26] Solid dispersion is considered to be the most suitable choice to improve dissolution rates and hence the bioavailability of the poorly water soluble drug. [27] However, the practical applicability of solid dispersion systems has remained limited due to difficulties in conventional methods of preparation, poor reproducibility of physiochemical properties, dosage formulation and lack of feasibility for scaling-up manufacturing processes. [28] Electrospun nanofibers may provide novel approaches as to how the dissolution rate of even very poorly soluble compounds might be improved to minimize the limitations of oral availability.…”

Section: Novel Strategies Provided By Electrospinning For New Ddsmentioning

confidence: 99%

Electrospun nanofiber-based drug delivery systems

Yu¹,

Zhu²,

White³

et al. 2009

Health

155

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Electrospinning is a very simple and versatile process by which polymer nanofibers with diameters ranging from a few nanometers to several micrometers can be produced using an electrostatically driven jet of polymer solution or polymer melt. Significant progress has been made in this process throughout the past few years and electrospinning has advanced its applications in many fields, including pharmaceutics. Electrospun nanofibers show great promise for developing many types of novel drug delivery systems (DDS) due to their special characteristics and the simple but useful and effective top-down fabricating process. The current state of electrospun nanofiber-based DDS is focused on drug-loaded nanofiber preparation from pharmaceutical and biodegradable polymers and different types of DDS. However, there are more opportunities to be exploited from the electrospinning process and the corresponding drug-loaded nanofibers for drug delivery. Additionally, some other related challenges and the possible resolutions are outlined in this review.

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“…Moreover, the proportion of the drug to the bulk matrix solid was also one of the critical parameters to critically affect the performance of SD (11). Other mechanisms might also exist to describe the performance of the carrier matrix in enhancing the dissolution of hydrophobic medications including conversion into less stable or distorted crystalline structure, amorphization, and attenuation of particle size to submicron or nano range and in improving the wettability of the drug by the dissolution medium (12). In this regard, the aim of our previously published study was to propose a solid dispersion formulation of sulpiride with an enhanced bioavailability after oral administration (10).…”

Section: Introductionmentioning

confidence: 99%

Pediatric Suppositories of Sulpiride Solid Dispersion for Treatment of Tourette Syndrome: In Vitro and In Vivo Investigations

et al. 2014

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Abstract. Pharmaceutical development was adopted in the current study to propose a pediatric rectal formulation of sulpiride as a substitute to the available oral or parenteral formulations in the management of Tourette syndrome (TS). The goal was to formulate a product that is easy to use, stable, and highly bioavailable and to achieve a rapid clinical efficacy. Towards this aim, sulpiride solid dispersion (SD) with tartaric acid at a weight ratio of 1:0.25 was incorporated into different suppository bases, namely witepsol W25, witepsol H15, witepsol E75, suppocire NA, suppocire A, glycerogelatin, and polyethylene glycols. The formulae were evaluated in vitro using different pharmacotechnical methods such as visual, melting, weight and content uniformities, drug release, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), and X-ray diffraction (XRD) analyses. In vivo bioavailability was also assessed in rabbits to compare the bioavailability of either raw sulpiride-incorporated or its SD-incorporated witepsol H15-based suppositories to its oral suspension (reference). Sulpiride SD-incorporated witepsol H15 formulation showed acceptable in vitro characteristics with a bioavailability of 117% relative to oral dosing, which excel that in humans (27% after dosing of oral product). In addition, the proposed formula not only passed the 6-month stability study but also proposed a promising scale-up approach. Hence, it showed a great potential for pediatric product development to manage TS in rural areas.

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Improving the Dissolution Rate of Poorly Water Soluble Drug by Solid Dispersion and Solid Solution—Pros and Cons

Cited by 118 publications

References 9 publications

In vitro and in vivo antitumor effect of gefitinib nanoparticles on human lung cancer

In vitro and in vivo antitumor effect of gefitinib nanoparticles on human lung cancer

Electrospun nanofiber-based drug delivery systems

Pediatric Suppositories of Sulpiride Solid Dispersion for Treatment of Tourette Syndrome: In Vitro and In Vivo Investigations

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