Pharmaceutical particles design by membrane emulsification: preparation methods and applications in drug delivery

© 2017 Bentham Science Publishers.Nowadays, the rational design of particles is an important issue in the development of pharmaceutical medicaments. Advances in manufacturing methods are required to design new pharmaceutical particles with target properties in terms of particle size, particle size distribution, structure and functional activity. Membrane emulsification is emerging as a promising tool for the production of emulsions and solidified particles with tailored properties in many fields. In this review, the current use of membrane emulsification in the production of pharmaceutical particles is highlighted. Membrane emulsification devices designed for small-scale testing as well as membrane-based methods suitable for large-scale production are discussed. A special emphasis is put on the important factors that contribute to the encapsulation efficiency and drug loading. The most recent studies about the utilization of the membrane emulsification for preparing particles as drug delivery systems for anticancer, proteins/peptide, lipophilic and hydrophilic bioactive drugs are reviewed

Polycaprolactone multicore-matrix particle for the simultaneous encapsulation of hydrophilic and hydrophobic compounds produced by membrane emulsification and solvent diffusion processes

Co-encapsulation of drugs in the same carrier, as well as the development of microencapsulation processes for biomolecules using mild operating conditions, and the production of particles with tailored size and uniformity are major challenges for encapsulation technologies. In the present work, a suitable method consisting of the combination of membrane emulsification with solvent diffusion is reported for the production of multi-core matrix particles with tailored size and potential application in multi-therapies. In the emulsification step, the production of a W/O/W emulsion was carried out using a batch Dispersion Cell for formulation testing and subsequently a continuous azimuthally oscillating membrane emulsification system for the scaling-up of the process to higher capacities. In both cases precise and gentle control of droplet size and uniformity of the W/O/W emulsion was achieved, preserving the encapsulation of the drug model within the droplet. Multi-core matrix particles were produced in a post emulsification step using solvent diffusion. The compartmentalized structure of the multicore-matrix particle combined with the different chemical properties of polycaprolactone (matrix material) and fish gelatin (core material) was tested for the simultaneous encapsulation of hydrophilic (copper ions) and hydrophobic (α-tocopherol) test components. The best operating conditions for the solidification of the particles to achieve the highest encapsulation efficiency of copper ions and α-tocopherol of 99 (±4)% and 93(±6)% respectively were found. The multi-core matrix particle produced in this work demonstrates good potential as a co-loaded delivery system

Microencapsulation of oil droplets using cold water fish gelatine/gum arabic complex coacervation by membrane emulsification

Food grade sunflower oil was microencapsulated using cold water fish gelatine (FG)–gum arabic (GA) complex coacervation in combination with a batch stirred cell or continuous pulsed flow membrane emulsification system. Oil droplets with a controllable median size of 40–240 μm and a particle span as low as 0.46 were generated using a microengineered membrane with a pore size of 10 μm and a pore spacing of 200 μm at the shear stress of 1.3–24 Pa. A biopolymer shell around the oil droplets was formed under room temperature conditions at pH 2.7–4.5 and a total biopolymer concentration lower than 4% w/w using weight ratios of FG to GA from 40:60 to 80:20. The maximum coacervate yield was achieved at pH 3.5 and a weight ratio of FG to GA of 50:50. The liquid biopolymer coating around the droplets was crosslinked with glutaraldehyde (GTA) to form a solid shell. A minimum concentration of GTA of 1.4 M was necessary to promote the crosslinking reaction between FG and GTA and the optimal GTA concentration was 24 M. The developed method allows a continuous production of complex coacervate microcapsules of controlled size, under mild shear stress conditions, using considerably less energy when compared to alternative gelatine types and production methods