Effect of Surfactants on the Melt Viscosity and Extent of Drug Embedment of Paraffin Wax Blends in Spray Congealing
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ORIGINAL ARTICLE
Effect of Surfactants on the Melt Viscosity and Extent of Drug Embedment of Paraffin Wax Blends in Spray Congealing Hongyi Ouyang 1 & Annabel Shi Yin Poh 1 & Paul Wan Sia Heng 1 & Lai Wah Chan 1 Accepted: 9 November 2020 # Springer Science+Business Media, LLC, part of Springer Nature 2020
Abstract Purpose Being hydrophobic, paraffin wax is potentially useful for developing taste-masked or sustained release drug formulations. However, its high hydrophobicity also makes it challenging to achieve good embedment of a hydrophilic drug (e.g. paracetamol) due to the significant interfacial tension experienced. While spray congealing is an efficient technique of producing microparticles for pharmaceutical applications, there has been limited investigation on the use of paraffin wax in this technique. Methods A rapid method based on microscopic assessment was developed to screen paraffin wax blends containing surfactants for good extent of drug embedment. The rheological properties of the molten blends were investigated. Suitable blends were spray-congealed and the products characterised. Statistical analysis of the data and drug release modelling were carried out. Results Drug-loaded paraffin wax was too viscous for spray congealing. The addition of surfactants decreased the melt viscosity and improved sprayability and microparticle yield. The microparticles showed high paracetamol encapsulation efficiency, with drug particles well-embedded in some formulations. The drug release was effected through diffusion and erosion of the matrix material. Conclusion The use of surfactants allowed successful embedment of paracetamol within spray-congealed microparticles, enabling taste-masking and sustained release. Keywords Paraffin wax . Spray congealing . Paracetamol . Surfactant . Viscosity . Microparticle
Introduction Poor patient compliance to medication regimen has been an issue that results in undesired disease progression, increased hospital admissions and a lower quality of life in patients [1]. Frequent administration of medications and unpleasant product taste [2–4] are two factors that commonly affect patient compliance. Many drugs are readily soluble, absorbed and metabolised, requiring administration several times a day [5]. Sustained release formulations can however be designed to achieve extended therapeutic effect by releasing the drug contents over a longer period of time [6]. Thus, these formulations can provide about 12 hourly coverage, therefore reducing the dosing frequency to twice a day and improving * Lai Wah Chan [email protected] 1
GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore
medication adherence [7]. Sustained release formulations, as well as taste-masked products, can be developed by embedding the drug in hydrophobic materials using an efficient technique of spray congealing. Spray congealing is a technique in which a hot molten mixture is sprayed into a cooled chamber
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