Optimising the release rate of naproxen liqui-pellet: a new technology for emerging novel oral dosage form

Abstract

Liqui-pellet is a new dosage form stemming from pelletisation technology and concept from liquisolid technology. In spite of liquipellet overcoming a major hurdle in liquisolid technology through achieving excellent flow property with high liquid load factor, the formulation requires to be optimised in order to improve drug release rate. Liqui-pellets of naproxen containing Tween 80, Primojel, Avicel and Aerosil were extruded and spheronised. Flowability test confirmed that all liqui-pellet formulations have excellent-good flow property (Carr's index between 3.9-11.17%), including liqui-pellets with a high liquid load factor of 1.52, where 38% of the total mass is co-solvent. This shows a relatively high liquid load factor can be achieved in liqui-pellet without compromising the flowability, which is one of the key novelty of this work. It was found that the improved drug release rate was due to the remarkably improved disintegration of the supposedly non-disintegrating microcrystalline-based pellet; the optimised liqui-pellet seems to explode into fragments in the dissolution medium. At pH 1.2, the optimised formulation had~10% more drug release than non-optimised formulation after 2 h, and at pH 7.4, the drug release of the optimised pellet was nearing 100% at~15 min, whereas the noneoptimised pellet only achieved~79% drug release after 2 h. DSC and XRPD indicated an increase in the dissolution rate could be due to molecularly dispersion of naproxen in the pellets. Overall results showed that liqui-pellet exhibited an enhanced drug release and the capacity for high liquid load factor whilst maintaining excellent flowability, rendering it a potentially commercially feasible drug delivery system.

Impact of Mucin on Drug Diffusion: Development of a Straightforward In Vitro Method for the Determination of Drug Diffusivity in the Presence of Mucin

“…However, the high variation in diffusion curves pointed out a reliability issue connected with the described setup, thus the one where the drug was dissolved in mucin and diffusing in water was solely applied. [19].…”

Solid Dispersion Pellets: An Efficient Pharmaceutical Approach to Enrich the Solubility and Dissolution Rate of Deferasirox

“…Recently, there has been a great trend and major attention in pharmaceutical research to the ways of enriching the dissolution percentage of low-soluble molecules [ 4 , 5 ]. Various strategies such as micro- and nanosizing, micelle formation, salt formation, complexation, liquisolids, liqui-pellets, and solid dispersion (SD) method have been exploited to enhance the dissolution rate and consequently improve the absorption of low-soluble agents at the gastrointestinal (GI) tract [ 6 – 8 ].…”

Liquisolid System and Liqui-Mass System Are Not the Same

“…There are formal records to support this claim. Later on, Liqui-Pellet was disclosed in a patent application in 2018 (9) followed by two publications in 2019 (5,6). The first two publications on Liqui-Pellet explains the fundamental difference between liquisolid system and liqui-mass system, which is crucial in giving Liqui-Pellet versatility and high liquid load factor, where~38% of the total mass of pellet is non-volatile co-solvent (6).…”

“…However, they are distinctively different in that they both use different systems (i.e. liqui-mass system versus liquisolid system)' (6) We note that Pezzini et al Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material.…”