Evidence map›Paper›PMID 40908687›Full record

ArticleAnti-inflammatory & anti-allergy agents in medicinal chemistry2025

Preparation and Evaluation of Amorphous Solid Dispersion of Etoricoxib, Employing A Fast Approach for Polymer Selection.

Bandenawaz M Shaikh, Jitendra W Gajbe, Ashwini R Madgulkar, Mangesh R Bhalekar, Minakshi B Shinde

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Article in Anti-inflammatory & anti-allergy agents in medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

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2 citing papers in PubMed.

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4 · The record

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5 · Who and what money

Authors and funding

5 authors.

Bandenawaz M ShaikhAll India Shri Shivaji Memorial Society's (AISSMS), College of Pharmacy, SPPU, Pune, India.ORCID 0009-0009-3593-7833
Jitendra W GajbeAll India Shri Shivaji Memorial Society's (AISSMS), College of Pharmacy, SPPU, Pune, India.ORCID 0000-0003-1346-9847
Ashwini R MadgulkarAll India Shri Shivaji Memorial Society's (AISSMS), College of Pharmacy, SPPU, Pune, India.ORCID 0000-0002-4693-6459
Mangesh R BhalekarAll India Shri Shivaji Memorial Society's (AISSMS), College of Pharmacy, SPPU, Pune, India.ORCID 0000-0003-0000-5859
Minakshi B ShindeAll India Shri Shivaji Memorial Society's (AISSMS), College of Pharmacy, SPPU, Pune, India.ORCID 0009-0006-0768-3854

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundNonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used to manage pain and inflammation but are associated with gastrointestinal and cardiovascular risks, especially with COX-2 inhibitors. Topical delivery systems offer a safer alternative by minimizing systemic exposure; however, poor solubility and limited skin penetration remain challenges. Enhancing solubility through solid dispersion and incorporating it into a gel formulation may improve permeability and therapeutic effectiveness, addressing the need for safer and more efficient topical NSAID delivery.

introductionThis investigation aimed to enhance the solubility and dissolution rate of poorly water-soluble etoricoxib through the development of solid dispersions using the kneading method.

methodsA suitable carrier was selected from a pool of candidates based on polarised microscopy analysis. The influence of a solubilizer on amorphization was evaluated. Solid dispersions of Etoricoxib and its corresponding physical mixtures, incorporating or excluding the solubilizer, were prepared at varying drug-to-carrier ratios. Yield, drug content, saturation solubility, and

resultsFTIR spectra indicated the formation of intermolecular hydrogen bonds within the dispersions. XRD, SEM, and DSC analysis confirmed the amorphous transition of crystalline etoricoxib in all the prepared solid dispersions. In comparison to pure etoricoxib and its physical mixes, the produced solid dispersions showed significantly improved dissolution and solubility, Discussion: Solid dispersion technology effectively enhanced the solubility and dissolution of poorly water-soluble etoricoxib. Polarised microscopy also proved valuable for rapid excipient screening. However, the study was limited by the narrow range of solubilizers tested. While Poloxamer 407 was selected for its availability and untapped potential, broader screening of advanced solubilizers could offer improved outcomes.

conclusionThe solubility increased from 99.08 to 296.8 μg/ml and the dissolution rose from 69.32% to 98.07%. These findings suggest that the kneading method and Poloxamer successfully produced amorphous solid dispersions of etoricoxib with significantly enhanced solubility and dissolution properties, potentially improving its bioavailability.

Indexed as

Anti-Inflammatory Agents, Non-SteroidalCyclooxygenase 2 InhibitorsEtoricoxibPolymersSulfonesCalorimetry, Differential ScanningChemistry, PharmaceuticalDrug CarriersDrug CompoundingSolubilitySpectroscopy, Fourier Transform InfraredX-Ray DiffractionAnti-Inflammatory Agents, Non-SteroidalCyclooxygenase 2 InhibitorsDrug CarriersEtoricoxibPolymersSulfonesamorphization.dissolution rateetoricoxibkneading methodSolid dispersionssolubility

Identifiers

PMID40908687

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.