Solid Dispersion of Hydroxypropyl β-Cyclodextrin and Ketorolac: Enhancement of In-vitro Dissolution Rates, Improvement in Anti-inflammatory Activity and Reduction in Ulcerogenicity in Rats

Objective: The current work was aimed to prepare a topical gel containing curcumin (CUR) for the treatment of microbial infections on skin. Methods: CUR was complexed with the β-cyclodextrin (β-CD) using kneading method in 1:1, 1:2, and 1:3 molar ratios and characterized. The inclusion complex with high aqueous solubility was loaded in the topical gel containing (2% CUR) which was prepared using carbopol, sodium CMC, and guar gum and evaluated for viscosity, spreadability, extrudability, pH, drug content, and in vitro diffusion studies. The in vitro anti-inflammatory activity of the gel was performed by albumin protein denaturation technique, the statistical analysis was done using ANOVA followed Dunnett’s t-test. The antimicrobial activity of CUR was evaluated using standard strains of Candida albicans and Escherichia coli by agar well diffusion method. Results: The complexation of CUR had an increased solubility up to 103.09 times for 1:3 molar ratio with in vitro dissolution 90.64% for 60 min. The optimized formulation F9 had viscosity of 6500.3 cps and 97.5% in vitro drug diffusion for 8 h which follows zero-order release kinetics. In vitro anti-inflammatory activity studied showed that the CUR gel has a good potency for renaturation and was as effective as standard diclofenac with 76.9% inhibition (p=0.0507). CUR showed approx. 3 mm diameter of zone of inhibition against C. albicans and E. coli. Conclusion: A stable topical gel of CUR using β-CD and carbopol was successfully prepared which showed better in vitro diffusion with promising anti-inflammatory and antifungal action.

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Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect

Oxidative Medicine and Cellular Longevity ◽

10.1155/2021/1818538 ◽

2021 ◽

Vol 2021 ◽

pp. 1-13

Author(s):

Abdulla Sherikar ◽

Mohd Usman Mohd Siddique ◽

Mahesh More ◽

Sameer N. Goyal ◽

Milan Milivojevic ◽

...

Keyword(s):

Solid Dispersion ◽

Solid Dispersions ◽

Biological Response ◽

Eutectic Mixture ◽

Fold Increase ◽

In Vitro Dissolution ◽

Anti Inflammatory ◽

Pvp K30

Solubility of phytochemicals is a major concern for drug delivery, permeability, and their biological response. However, advancements in the novel formulation technologies have been helping to overcome these challenges. The applications of these newer technologies are easy for commercialization and high therapeutic outcomes compared to conventional formulations. Considering these facts, the present study is aimed to prepare a silymarin-loaded eutectic mixture with three different ratios of Polyvinylpyrrolidone K30 (PVP K30) and evaluating their anti-inflammatory, and hepatoprotective effects. The preliminary phytochemical and characterization of silymarin, physical mixture, and solid dispersions suggested and successfully confirmed the formation of solid dispersion of silymarin with PVP K30. It was found that the solubility of silymarin was increased by 5-fold compared to pure silymarin. Moreover, the in vitro dissolution displayed that 83% of silymarin released within 2 h with 2.8-fold increase in dissolution rate compared to pure silymarin. Also, the in vivo study suggested that the formulation significantly reduced the carbon tetrachloride- ( 0.8620 ± 0.05034 ∗ ∗ for 1 : 3 ratio), paracetamol- ( 0.7300 ± 0.01517 ∗ ∗ for 1 : 3 ratio), and ethanol- ( 0.8100 ± 0.04037 ∗ ∗ for 1 : 3 ratio) induced hepatotoxicity in rats. Silymarin solid dispersion was prepared using homogenization methods that have prominent anti-inflammatory effect ( 0.6520 ± 0.008602 ∗ ∗ with 8.33%) in carrageenan-induced rat paw model.

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Improving the in vivo bioavailability and in vitro anti-inflammatory activity of tanshinone IIA by alginate solid dispersion

Journal of Drug Delivery Science and Technology ◽

10.1016/j.jddst.2020.101966 ◽

2020 ◽

Vol 60 ◽

pp. 101966 ◽

Cited By ~ 1

Author(s):

Chao Luo ◽

Weibin Wu ◽

Shuaijie Lou ◽

Saiqi Zhao ◽

Kai Yang

Keyword(s):

Solid Dispersion ◽

Tanshinone Iia ◽

Inflammatory Activity ◽

Anti Inflammatory

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Evaluation of the Solid Dispersion System Engineered from Mesoporous Silica and Polymers for the Poorly Water Soluble Drug Indomethacin: In Vitro and In Vivo

Pharmaceutics ◽

10.3390/pharmaceutics12020144 ◽

2020 ◽

Vol 12 (2) ◽

pp. 144 ◽

Cited By ~ 1

Author(s):

Ziyue Xi ◽

Wei Zhang ◽

Yali Fei ◽

Mingshu Cui ◽

Luyao Xie ◽

...

Keyword(s):

Mesoporous Silica ◽

Solid Dispersion ◽

In Vitro Release ◽

Water Soluble ◽

In Vitro Dissolution ◽

Membrane Penetration ◽

Artificial Membrane ◽

Dissolution Rates

This work explored absorption efficacy via an in vivo imaging system and parallel artificial membrane penetration in indomethacin (IMC) solid dispersion (SD) systems. Two different polymer excipients—hydroxypropyl methylcellulose (HPMC) and Kollicoat IR as precipitation inhibitors (PIs)—combined with mesoporous silica nanoparticles (MSNs) as carriers were investigated. The IMC–SDs were prepared using the solvent evaporation method and characterized by solubility analysis, infrared (IR) spectroscopy, powder X-ray diffraction (PXRD), field emission scanning electron microscopy (FESEM), and differential scanning calorimetry (DSC). It was confirmed that IMC successfully changed into an amorphous state after loading into the designed carriers. The in vitro release and stability experiments were conducted to examine the in vitro dissolution rates of IMC–SDs combined with HPMC and Kollicoat IR as PIs which both improved approximately three-fold to that of the pure drug. Finally, in vivo studies and in vitro parallel artificial membrane penetration (PAMPA) experiments ensured the greater ability of enhancing the dissolution rates of pure IMC in the gastrointestinal tract by oral delivery. In brief, this study highlights the prominent role of HPMC and Kollicoat IR as PIs in MSN SD systems in improving the bioavailability and gastrointestinal oral absorption efficiency of indomethacin.

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Formulation of Ketoprofen Transdermal Solid Dispersion Patch as an Analgesic and Anti-Inflammatory

Asian Journal of Pharmaceutical Research and Development ◽

10.22270/ajprd.v8i3.760 ◽

2020 ◽

Vol 8 (3) ◽

pp. 51-58

Author(s):

Fitri Yani ◽

Anayanti Arianto ◽

Rosidah Noersal

Keyword(s):

Propylene Glycol ◽

Solid Dispersion ◽

Physicochemical Characteristics ◽

Inflammatory Activity ◽

Penetration Testing ◽

Transdermal Patches ◽

Anti Inflammatory ◽

Diffraction Patterns ◽

Inflammatory Effect

Objective: to formulate transdermal patches of ketoprofen solid dispersions, determine the effect of propylene glycol on the rate of release of ketoprofen transdermal solid dispersion patches to know the optimum transdermal patch form of a solid dispersion of ketoprofen could provided better analgesic and antiinflammatory effects compared to the trademark ketoprofen gel (Kaltrofen®). Design: this research was conducted using a transdermal experiment of dense solid dispersion patches of ketoprofen with variations in the amount of propylene glycol F1 (10%), F2 (20%) and F3(30%) , physicochemical characteristics (organoleptic, fiber, weight uniformity, folding enhancement and development), diffraction patterns (XRD), incompatibility patterns (FTIR), in vitro penetration testing. -vitro, evaluation of analgesic and anti-inflammatory activity. Interventions: the intervened variable were the in vitro penetration testing. In-vitro, evaluation of analgesic and anti-inflammatory effect of ketoprofen transdermal solid dispersion patch. Main outcome measures: the main measurement in this study were physicochemical characteristics (organoleptic, fiber, weight uniformity, folding enhancement and development), diffraction patterns (XRD), incompatibility patterns (FTIR), in vitro penetration testing. -vitro, evaluation of analgesic and anti-inflammatory activity. Results: transdermal patches of ketoprofen solid dispersion patches produce white, odorless preparations that have a flat surface, thickness between 0.0242 ± 0.0002 to 0.0269 ± 0.0003, weight uniformity 321.50 ± 0.78 to 381.54 ± 0.60, folding resistance between 375 ± 0.58 to 443 ± 1.53, all formulas already meet the requirements of physicochemical characteristics. F3 ketoprofen transdermal solid dispersion patch had a highest penetration degree and provide better analgesic effects compared to the trademark ketoprofen gel (Kaltrofen®), and there were significant differences between groups (p>0.05). Conclusion: it can be concluded that the use of 30% propylene glycol in F3 ketoprofen transdermal solid dispersion patch affects the rate of drug release and had a better anti-inflammatory effect compared to the trademark ketoprofen gel (Kaltrofen®).

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