Physicochemical investigation of the solid dispersion systems of etoricoxib with poloxamer 188

Karekar, Poonam; Vyas, Vikrant; Shah, Manali; Sancheti, Pankajkumar; Pore, Yogesh

doi:10.1080/10837450802683974

Cited by 25 publications

(16 citation statements)

References 35 publications

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“…Amid amphiphilic polymers, poloxamers are nonionic polyoxyethylene-polypropylene block copolymer consisting of hydrophilic core (ethylene oxide) and hydrophobic core (polypropylene oxide) have been widely used to improve the solubility of poorly soluble drugs [ 12 , 25 ]. Generally the mechanism of improvement of solubility is observed due to its wetting and surface adsorbing properties as well as low melting point [ 26 ]. On the other hand, Eudragit® polymers are poly (methacrylic acid-co-methyl methacrylate) derivatives, well known for their solubilizing and sustained delivery properties and hence could be a potential carrier for SRSDs [ 21 , 27 ].…”

Section: Introductionmentioning

confidence: 99%

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Halder

Ahmed

Shuma

et al. 2020

Heliyon

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Purpose The present study aimed to develop carvedilol (CAR)-loaded (25% w/w) sustained release solid dispersion (SRSD), for enhanced dissolution and to explore the applicability of different industrially accessible drying techniques. Methods SRSD-CAR containing different ratios of polymers were prepared and physicochemically characterized. Dissolution study was carried out in both sink and supersaturated conditions to identify the possible enhancement in dissolution behavior. Results Based on the solubility study, Kolliphor® P188 and Eudragit® RSPO (50:25, % w/w) ratio exhibited the highest solubility among the samples and was chosen as the optimal composition of SRSD-CAR for further characterization. The crystallinity assessments of the optimized formulation indicated amorphization of CAR in the formulation, bring about improved solubility of CAR. The infrared spectroscopic study revealed minor transitions; demonstrating the absence of significant interactions between drug and carrier. Furthermore, the SRSD-CAR exhibited immediate formation of nano particles when dispersed in water. Dissolution study revealed significant improvement in dissolution behavior, with a release of CAR in a gradual manner compared to crystalline CAR. From the dissolution kinetics analysis, the Korsmeyer Peppas model fit the best and diffusion was predominant in release of CAR. The drug release pattern showed insignificant differences between the SRSD-CAR formulations prepared by rotary vacuum drying and freeze drying. Conclusion From these experimental findings, SRSD approach might be a favorable dosage option for CAR, offering improved biopharmaceutical properties.

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Section: Introductionmentioning

confidence: 99%

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Halder

Ahmed

Shuma

et al. 2020

Heliyon

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“…Therefore, improvements in solubility and/or dissolution rate of etoricoxib may be achieved through the preparation of solid dispersions. In the literature, various solid dispersions of etoricoxib are reported for improving the dissolution of etoricoxib using various carriers like polyvinyl pyrrolidone K 30 (PVP K 30) [10], polyethylene glycol 4000 (PEG 4000) and polyvinyl pyrrolidone K 30 (PVP K 30) combination [11], Poloxamer 188 [12], and Gelucire 50/13, Compritol, and Sterotex K NF [13]. In the literature, various solid dispersions using sugars as carriers are reported [14–21].…”

Section: Introductionmentioning

confidence: 99%

Solubility and Dissolution Enhancement of Etoricoxib by Solid Dispersion Technique Using Sugar Carriers

et al. 2011

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The aim of the present study was to improve solubility and dissolution of the poorly aqueous soluble drug, etoricoxib by solvent evaporation technique using various sugar carriers, such as lactose, sucrose, and mannitol. Etoricoxib solid dispersions and their respective physical mixtures using lactose, sucrose, and mannitol were prepared in different ratios by solvent evaporation technique. The percent yield, drug content, saturation solubility, and in vitro dissolution of etoricoxib solid dispersions and physical mixtures were analyzed. Etoricoxib solid dispersions were characterized by FTIR spectroscopy, XRD, and DSC analysis. The FTIR spectroscopic analysis revealed the possibility of intermolecular hydrogen bonding in various solid dispersions. The XRD and DSC studies indicated the transformation of crystalline etoricoxib (in pure drug) to amorphous etoricoxib (in solid dispersions) by the solid dispersion technology. Both the aqueous solubility and dissolution of etoricoxib were observed in all etoricoxib solid dispersions as compared with pure etoricoxib and their physical mixtures. The in vitro dissolution studies exhibited improved dissolution in case of solid dispersion using lactose than the solid dispersions using both sucrose and mannitol. The in vitro dissolution of etoricoxib from these solid dispersions followed Hixson-Crowell model.

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“…5 ml of samples were withdrawn at appropriate time intervals. The volume of dissolution media was adjusted to 900 ml by replacing each 5 ml aliquot withdrawn with 5 ml of fresh phosphate buffer (pH 7.4) [21]. The solution was immediately filtered through membrane filter paper 0.2 µm, and adequately diluted if necessary and analyzed spectrophotometrically at 288 nm (Shimadzu 1800, Japan).…”

Section: In Vitro Drug Releasementioning

confidence: 99%

“…Insptite of powerful analgesic and anti-inflammatory potential [17,18], ECB exhibits a delayed rate of absorption [17]. Therefore, efforts were made to improve the physicochemical properties of ECB using solid dispersion [19][20][21], drug amorphization [22][23][24], cyclodextrin complexation [25,26] and spherical crystallization technique [27]. In this article, the formation of nanocomposites of ECB were attempted with Soluplus ® to evaluate it for physicochemical properties as well as anti-inflammatory activity.…”

Section: Introductionmentioning

confidence: 99%

Preparation, Characterization, and Evaluation of Anti-Inflammatory Activity of Etoricoxib Loaded Soluplus® Nanocomposites

Pore¹,

Mane²,

Mangrule³

et al. 2018

Int J App Pharm

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Objective: The objective of this study was to prepare and characterize etoricoxib (ECB) loaded Soluplus® nanocomposites to improve its physicochemical properties. The effect of polymer and surfactant concentration on particle size, in vitro percentage dissolution efficiency and the anti-inflammatory activity of nanocomposites were also investigated.Methods: The nanocomposites were prepared by using a freeze-drying technique. The analytical evidence for the formulation of lyophilized nanocomposites in solid state were generated and confirmed by differential scanning calorimetry (DSC), fourier transformation infrared spectroscopy (FTIR), x-ray powder diffractometry (XPRD) and scanning electron microscopy (SEM). The in vitro drug release profile of nanocomposites was compared with pure ECB powder.Results: The nanocomposites of ECB were contained in a nano range with particle size and zeta potential of 63.5 nm and 46.5 mv, respectively. The solubility and dissolution of the nanocomposites were significantly (p<0.001) improved as compared to ECB alone, evidenced by decreased log P values (1.90±0.002) of the nanocomposites. The characterization studies revealed the formation of amorphous nanocomposites of ECB with existence of physical interactions between drug and polymer. The anti-inflammatory activity of nanocomposites evaluated by carrageenan-induced rat paw edema model demonstrated nonsignificant (p>0.05) increase in anti-inflammatory activity as compared to pure ECB.Conclusion: From the results, it could be concluded that the formation of ECB nanocomposites with Soluplus® could be an effective and alternative approach to modify the physicochemical properties of ECB.

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Physicochemical investigation of the solid dispersion systems of etoricoxib with poloxamer 188

Cited by 25 publications

References 35 publications

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Solubility and Dissolution Enhancement of Etoricoxib by Solid Dispersion Technique Using Sugar Carriers

Preparation, Characterization, and Evaluation of Anti-Inflammatory Activity of Etoricoxib Loaded Soluplus® Nanocomposites

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