Deciphering the Role of Plasticizers and Solvent Systems in Hydrophobic polymer coating on Hydrophilic core

Abstract

The type of plasticizer and the choice of solvent or co-solvents used for coating of a hydrophilic core can greatly impact the permeability, porosity, and mechanical strength of the polymer film. Although, Ethylcellulose (EC) is an old polymer, it is a polymer of choice for modifying the drug release due to its inherent properties. The ability of polymers like EC alone to form a diffusion-controlling membrane with good mechanical properties is limited. To modulate the drug release as per the desired profile and modify the film properties, ethylcellulose is often used with hydrophilic hypromellose (HPMC) along with plasticizers. The main focus of the current study was the identification of an appropriate solvent system and plasticizer for the ethylcellulose-hypromellose polymer combination. The study evaluated the coating solution properties, the feasibility and efficiency of the process, the physical attributes of the tablet, the surface properties of the polymer film, the in-vitro drug release and behavior, and the impact of curing time on surface properties and drug release, among other factors.

The isopropyl alcohol-water mixture (9:1) produced a homogeneous film in comparison to films produced by other solvents. Although both hydrophilic and hydrophobic plasticizers produce homogeneous films, hydrophilic plasticizers have a higher rate of drug diffusion than hydrophobic plasticizers. During the tablet curing and stability study, the drug release from the polymeric film coating with triethyl citrate decreased moderately and with polyethylene glycol decreased significantly. The presence of hydrophobic plasticizers, viz., dibutyl sebacate and acetyl tributyl citrate, in the polymeric film coating does not impact drug release. For the combination of ethylcellulose and hypromellose, it was found that a mixture of isopropyl alcohol and water (9:1) worked better as a solvent for coating solutions, and hydrophobic plasticizers lower the risk associated with coating ethylcellulose and hypromellose together.

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Materials

Metformin HCl (grade: USP; manufacturer: USV), lactose monohydrate (grade: Pharmatose® 200M; manufacturer: DFE), povidone (grade: Kollidon® 30; manufacturer: BASF), colloidal silicon dioxide (grade: Aerosil 200 pharma; manufacturer: Evonik), magnesium stearate (grade: Ligamed MF-2-V; manufacturer: Petergreven), hypromellose (grade: AnycoatC AN-5; manufacturer: Lotte), ethylcellulose (grade: Ethocel Standard 10 Premium; manufacturer: Dupont), TEC (manufacturer: Vertellus), PEG (grade: Kollisolv® PEG 400; manufacturer: BASF), DBS (manufacturer: Vertellus), ATBC (manufacturer: Vertellus) was obtained from Centaur Pharmaceuticals. Hydrochloric acid (37 %), sodium hydroxide, potassium dihydrogen phosphate, disodium hydrogen phosphate, sodium acetate, glacial acetic acid of analytical grade (Emparta®; manufacturer: Merck)

Deepak Khobragade, Pramod Parshuramkar, Surendra Agrawal, Rahul Ingale, Mrunali Potbhare, Deciphering the Role of Plasticizers and Solvent Systems in Hydrophobic polymer coating on Hydrophilic core, HELIYON, https://doi.org/10.1016/j.heliyon.2024.e37938

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