Optimization of a Combined Wet Milling Process in Order to Produce Poly(vinyl Alcohol) Stabilized Nanosuspension

Overview

Journal Drug Des Devel Ther

Specialty Pharmacology

Date 2018 Jun 19

PMID 29910603

Citations 5

Authors

Csaba Bartos

Orsolya Jojart-Laczkovich

Gabor Katona

Maria Budai-Szucs

Rita Ambrus

Alexandra Bocsik

Ilona Grof

Maria Anna Deli

Piroska Szabo-Revesz

Affiliations

Soon will be listed here.

Abstract

Purpose: The article reports a wet milling process, where the planetary ball mill was combined with pearl milling technology to reach nanosize range of meloxicam (Mel; 100-500 nm). The main purpose was to increase the dissolution rate and extent of a poorly water-soluble Mel as nonsteroidal anti-inflammatory drug as well as to study its permeability across cultured intestinal epithelial cell layers.

Methods: Viscosity of milled dispersion and particle size distribution and zeta potential of Mel were investigated and differential scanning calorimeter and X-ray powder diffractometer were used to analyse the structure of the suspended Mel. Finally in vitro dissolution test and in vitro cell culture studies were made.

Results: It was found that the ratio of predispersion and pearls 1:1 (w/w) resulted in the most effective grinding system (200-fold particle size reduction in one step) with optimized process parameters, 437 rpm and 43 min. Nanosuspension (1% Mel and 0.5% poly[vinyl alcohol]) as an intermediate product showed a stable system with 2 weeks of holding time. This optimized nanosuspension enhanced the penetration of Mel across cultured intestinal epithelial cell layers without toxic effects.

Conclusion: The dissolution rate of Mel from the poly(vinyl alcohol) stabilized nanosuspension justified its applicability in the design of innovative per oral dosage form (capsule) in order to ensure/give a rapid analgesia.

Citing Articles

Study on the Scale-Up Possibility of a Combined Wet Grinding Technique Intended for Oral Administration of Meloxicam Nanosuspension.

Bartos C, Motzwickler-Nemeth A, Kovacs D, Burian K, Ambrus R Pharmaceutics. 2025; 16(12.

PMID: 39771492 PMC: 11680036. DOI: 10.3390/pharmaceutics16121512.

Optimization of Glyburide-loaded Nanosuspensions Ball Milling and Homogenization Techniques: A Central Composite Design Approach for Enhanced Solubility.

Gungor D, Aytekin E, Akdag Y, Sahin S, Gulsun T Curr Pharm Des. 2024; 31(5):377-390.

PMID: 39313907 DOI: 10.2174/0113816128321501240828054050.

Examine stability polyvinyl alcohol-stabilized nanosuspensions to overcome the challenge of poor drug solubility utilizing molecular dynamic simulation.

Abdollahi S, Raissi H, Farzad F Sci Rep. 2024; 14(1):17386.

PMID: 39075104 PMC: 11286956. DOI: 10.1038/s41598-024-68362-2.

Combination of Dissolving Microneedles with Nanosuspension and Co-Grinding for Transdermal Delivery of Ketoprofen.

Ramadon D, Ulayya F, Qurani A, Iskandarsyah I, Harahap Y, Anjani Q Pharmaceuticals (Basel). 2023; 16(3).

PMID: 36986478 PMC: 10054238. DOI: 10.3390/ph16030378.

Smartcrystals for Efficient Dissolution of Poorly Water-Soluble Meloxicam.

Ambrus R, Alshweiat A, Szabo-Revesz P, Bartos C, Csoka I Pharmaceutics. 2022; 14(2).

PMID: 35213978 PMC: 8879336. DOI: 10.3390/pharmaceutics14020245.

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