Investigation of Drug–Polymer Miscibility and Solubilization on Meloxicam Binary Solid Dispersion

Shi, Xiangjun; Huang, Wan; Xu, Tiantian; Fan, Baibai; Sheng, Xiaoxia

doi:10.1007/s12247-019-09378-4

Cited by 11 publications

(5 citation statements)

References 41 publications

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“…The addition of these penetration enhancers influences the thermodynamic activity of MX in the delivery system [31]. PVP is a suitable additive that reduces the particle size to nanometers and prevents the aggregation of nanoparticles, increasing the MX solubility [33,36,37]. PEG is a biocompatible polymer able to enhance the dissolution rate of poor water-soluble drugs due to its hydrophilic and lipophilic properties [38,39].…”

Section: Resultsmentioning

confidence: 99%

“…According to the literature, the PVP addition determines a weak ondary bonding between MX and PVP (according to FTIR spectra presented in Figu and 7 from Ref. [34]), whereas MX exhibits a high and fast dissolution rate in PVP-b formulations [33,37].…”

Section: Rheological Behavior 221 Temperature-induced Gelation Monito...mentioning

confidence: 95%

“…PVP chains have a stronger enthalpy of adsorption to micellar corona as compared with PEG [48]; thus, the destabilization of the PU network structure is higher, as can be seen from rheological data. However, both excipients, PEG and PVP are recommended as adsorption enhancers for MX [33,37]. As a result, the composition of Sample 3 was optimized by incorporating a PEG/PVP mixture in the PU sol state.…”

Section: Self-healing Behaviormentioning

confidence: 99%

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Thermosensitive Polyurethane-Based Hydrogels as Potential Vehicles for Meloxicam Delivery

Plugariu,

Gradinaru,

Avadanei

et al. 2023

Pharmaceuticals

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Meloxicam (MX) is a nonsteroidal anti-inflammatory drug (NSAID) used mainly to reduce pain, inflammation, and fever. In the present study, thermosensitive polyurethane (PU)-based hydrogels with various excipients (PEG, PVP, HPC, and essential oil) were prepared and loaded with MX. Rheological investigations were carried out on the PU-based formulations in various shear regimes, and their viscoelastic characteristics were determined. The average size of the PU micelles was 35.8 nm at 37 °C and slightly increased at 37 nm in the presence of MX. The zeta potential values of the hydrogels were between −10 mV and −11.5 mV. At pH = 6 and temperature of 37 °C, the formulated PU-based hydrogels loaded with MX could deliver significant amounts of the active substance, between 60% and 80% over 24–48 h and more than 90% within 2 weeks. It was found that anomalous transport phenomena dominated MX’s release mechanism from the PU-based networks. The results are encouraging for further studies aiming to design alternative carriers to commercial dosage forms of nonsteroidal anti-inflammatory drugs.

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Section: Resultsmentioning

confidence: 99%

Section: Rheological Behavior 221 Temperature-induced Gelation Monito...mentioning

confidence: 95%

Section: Self-healing Behaviormentioning

confidence: 99%

See 1 more Smart Citation

Thermosensitive Polyurethane-Based Hydrogels as Potential Vehicles for Meloxicam Delivery

Plugariu,

Gradinaru,

Avadanei

et al. 2023

Pharmaceuticals

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show abstract

“…• Poor membrane permeability: Some drugs, even if soluble, may have difficulty passing through the intestinal membranes and entering the bloodstream [3,4].…”

Section: Improving Oral Bioavailability Of Meloxicam: Development And...mentioning

confidence: 99%

“…This study focuses on overcoming this challenge by improving the solubility and dissolution rate of a specific poorly soluble drug.When administered orally, a drug needs to dissolve in the stomach or intestines before it can be absorbed through the GI tract and reach systemic circulation [6,7]. Drugs with poor aqueous solubility often exhibit limited absorption due to slow dissolution rates.Enhancing Solubility and Dissolution Rate: This approach targets poorly soluble drugs by increasing their solubility and dissolution rate in aqueous solutions, thereby facilitating better absorption [8].…”

Section: Improving Oral Bioavailability Of Meloxicam: Development And...mentioning

confidence: 99%

Improving Oral Bioavailability of Meloxicam: Development and Characterization of Solid Dispersions

Ratan,

Malik,

Singh

et al. 2024

JBPR

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This study investigated the development of a solid dispersion to improve the solubility and dissolution of meloxicam, a poorly water-soluble drug. Meloxicam is used to treat pain and inflammation in various conditions. The challenge was to enhance the drug's oral bioavailability by overcoming its low solubility. Two approaches were explored: 1. Kneading method with Poloxamer 407: This method resulted in a formulation with significantly improved solubility compared to the pure drug. Solvent evaporation method with PVP K-30: While this method offered satisfactory solubility enhancement, it was not as effective as the kneading method with Poloxamer 407.Following the development of the optimized solid dispersion, a suspension formulation was prepared using various suspending agents. The optimized drug formula was then incorporated into the suspension mix. Characterization studies confirmed compatibility between the drug and excipients. FT-IR analysis showed no interaction between the drug and the carriers. Scanning electron microscopy (SEM) revealed a change in meloxicam particle morphology from crystalline to a more amorphous form, indicating a reduction in particle size and a potential explanation for the improved dissolution profile. The dissolution profile of the solid dispersion suspension prepared by the kneading method with Poloxamer 407 outperformed the one prepared with the solvent evaporation method and PVP K-30.This study demonstrates the effectiveness of the kneading method with Poloxamer 407 in developing a solid dispersion of meloxicam with enhanced solubility and dissolution. The optimized formulation exhibited good stability, acceptable drug content and release, and satisfactory rheological properties. This approach has the potential to improve the bioavailability of meloxicam and lead to a more effective oral dosage form. Keywords: Oral Bioavailability, Meloxicam:, Solid Dispersions , FT-IR analysis, SEM

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Systematic screening of pharmaceutical polymers for hot melt extrusion processing: a comprehensive review

Thakkar

Pillai

et al. 2020

International Journal of Pharmaceutics

103

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Investigation of Drug–Polymer Miscibility and Solubilization on Meloxicam Binary Solid Dispersion

Cited by 11 publications

References 41 publications

Thermosensitive Polyurethane-Based Hydrogels as Potential Vehicles for Meloxicam Delivery

Thermosensitive Polyurethane-Based Hydrogels as Potential Vehicles for Meloxicam Delivery

Improving Oral Bioavailability of Meloxicam: Development and Characterization of Solid Dispersions

Systematic screening of pharmaceutical polymers for hot melt extrusion processing: a comprehensive review

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