Applications of hot-melt extrusion for drug delivery

Abstract

In today’s pharmaceutical arena, it is estimated that more than 40% of new chemical entities produced during drug discovery efforts exhibit poor solubility characteristics. However, over the last decade hot-melt extrusion (HME) has emerged as a powerful processing technology for drug delivery and has opened the door to a host of such molecules previously considered unviable as drugs. HME is considered to be an efficient technique in developing solid molecular dispersions and has been demonstrated to provide sustained, modified and targeted drug delivery resulting in improved bioavailability. This article reviews the myriad of HME applications for pharmaceutical dosage forms such as tablets, capsules, films and implants for drug delivery through oral, transdermal, transmucosal, transungual, as well as other routes of administration. Interest in HME as a pharmaceutical process continues to grow and the potential of automation and reduction of capital investment and labor costs have made this technique worthy of consideration as a drug delivery solution.

Influence of Process and Formulation Parameters on Dissolution and Stability Characteristics of Kollidon® VA 64 Hot-Melt Extrudates

“…A myriad of techniques such as spray drying [2], solvent evaporation [3], nanocrystal formation [4], complexation [5], and micronization of active pharmaceutical ingredient (API) [6] have been widely utilized in the industry to improve the solubility and/or dissolution rate of such BCS class II drugs, thereby enhancing their bioavailability. During the past couple of decades, hot-melt extrusion (HME) technology has gained enormous interest among researchers for improving the bioavailability of drug substances, especially those having low water solubility, by the formation of solid dispersions [7][8][9]. Compared to other techniques, HME offers several advantages such as being solvent-free, a potentially continuous process, and involving fewer processing steps in general.…”

In-line NIR spectroscopy for the understanding of polymer–drug interaction during pharmaceutical hot-melt extrusion

“…Recently, it also found its application in pharmaceutical manufacturing operations, offering many advantages compared to traditional pharmaceutical processing techniques [1][2][3][4][5] for solids: the process is anhydrous; poorly compactable materials can be incorporated into tablets; the materials have a short residence time in the extruder during processing; HME enables superior mixing (both distributive and dispersive); it allows the production of formulations with modified release; it allows masking of the bitter taste of several active pharmaceutical ingredients (API's) and in addition it improves the dissolution rate and the bioavailability of poorly water soluble drugs by the formation of solid solutions or solid dispersions [6] . A solid dispersion consists of at least two different components, generally a hydrophilic matrix and a hydrophobic drug [7] .…”

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

“…Polymethacrylates are widely used in pharmaceutical delivery systems for sustained drug delivery, 10) hot melt extrusion, 11,12) microencapsulation, 13) nanoparticle, 14,15) antiretroviral drug delivery, 15,16) floating microspheres, 17) colon delivery 18,19) and transdermal drug delivery. 20) In our previous studies we showed the effect of thermal treating on the release of indomethacin 8) and diclofenac sodium 9) from acrylic matrix tablets and mechanistically studied the effect of heat-treating on physicochemical structure of tablet.…”