International Journal of Drug Delivery Technology
Volume 14, Issue 1

Solubility Enhancement of Poorly Water-Soluble Aceclofenac by Amalgamation Micronization and Solid Dispersion Techniques

Vishal Gupta1*, Sokindra Kumar1, Rajesh Agrawal2

1Faculty of Pharmacy, Swami Vivekanand Subharti University, Meerut, Uttar Pradesh, India.

2GM – Research and Development Lab, Modi-Mundipharma Pvt. Ltd., Meerut, Uttar Pradesh, India. 

Received: 28th July, 2023; Revised: 31st January, 2024; Accepted: 06th March, 2024; Available Online: 25th March, 2024

ABSTRACT

Aceclofenac is a poorly aqueous soluble Biopharmaceutical Classification System (BCS) class II drug that has bioavailability problems after oral administration due to low aqueous solubility. There are numerous solubility modification approaches and they also have process limitations. Hence, the present research work aims to use two different solubility enhancement techniques (Micronization with Solid dispersion) simultaneously to counter individual limitations of techniques. The micronization technique increases the solubility of pure aceclofenac through increasing particle surface area, but it produces charged micronized material, leading to segregation and clumping of micronized material. Hence, micronized material handling during dosage form manufacturing is quite difficult. In the present research work, aceclofenac material is micronized by air jet mill to produce materials of below 25 µm size ranges. This micronized aceclofenac material is further encapsulated in a solid dispersion technique to produce amorphous aceclofenac materials. Solid dispersion of micronized aceclofenac was prepared by various techniques like physical kneading, solvent evaporation, melting and a combination thereof using different polymers (Polyox 301, HPMC, cetostearyl alcohol and glyceryl behenate). The prepared solid dispersion formulation (SD-31, SD-22, SD-23 and SD-30) exhibited an increase in the dissolution of aceclofenac as compared to pure aceclofenac. Various characterization techniques (Differential scanning calorimetry (DSC), X-ray Diffraction (XRD) and scanning electron microscope (SEM)) also reveal that aceclofenac crystallinity is significantly minimized in Solid dispersion formulation of SD-31, SD-22, SD-23 and SD-30. This selected solid dispersion (SD-31 and SD-22) also exhibited good stability (Photostability and stability at 40°C/75% RH after 3 months).

Keywords: BCS class, Solubility enhancement, Micronization, Solid dispersion, Aceclofenac, Stability. International Journal of Drug Delivery Technology (2024); DOI: 10.25258/ijddt.14.1.16

How to cite this article: Gupta V, Kumar S, Agrawal R. Solubility Enhancement of Poorly Water-Soluble Aceclofenac by Amalgamation Micronization and Solid Dispersion Techniques. International Journal of Drug Delivery Technology. 2024;14(1):109-117.

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