Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

Abstract

Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

Characterization and Release Behavior of a Thiosemicarbazone from Electrospun Polyvinyl Alcohol Core-Shell Nanofibers

“…Drug solubility and bioavailability are the serious challenges in the field of pharmaceuticals formulation [ 22 , 23 , 24 , 25 , 26 ]. Especially for hydrophobic drugs, solubility improvement is the key issue in the development of formulations [ 23 ].…”

“…Drug solubility and bioavailability are the serious challenges in the field of pharmaceuticals formulation [ 22 , 23 , 24 , 25 , 26 ]. Especially for hydrophobic drugs, solubility improvement is the key issue in the development of formulations [ 23 ]. Several solubility improvement methods such as solid dispersion, complexation, lipid-based systems, micronization, nanonization, and co-crystallization have been reported for improving the solubility and bioavailability of poorly water-soluble drugs [ 27 ].…”

“…The electrospinning method represents a combination of solid dispersion technology and nanotechnology. In this method, solid fibers in the micro- or nanometer range are produced from a polymeric fluid stream or melt delivered through a millimeter-scale nozzle [ 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 ]. In the pharmaceutical field, electrospinning has recently gained high interest for the production of drug delivery systems based on nanofibers [ 31 , 32 , 33 , 34 , 35 ].…”

Nanoencapsulation of Plant Volatile Organic Compounds to Improve Their Biological Activities

“…Nanoencapsulation of plant VOCs can decrease the volatility of bioactive compounds, protect them from external factors such as oxygen, light, moisture, and pH, and increase their solubilities. Encapsulated plant VOCs are likely to possess higher biological activities than free compounds, as the nanoparticles can mediate the controlled release and increased cellular accessibility of the volatiles [106].…”

Preparation of solid dispersion of rutin by spay drying

“…Trong đó, dược chất ít tan được phân tán vào trong chất mang và tồn tại dưới dạng các phân tử riêng biệt, các hạt vô định hình, hoặc các hạt tinh thể. Hiện nay có rất nhiều phương pháp để bào chế hệ phân tán rắn như đun chảy, nghiền, dùng dung môi siêu tới hạn, phun sấy, bốc hơi dung môi, đùn nóng chảy, kỹ thuật đông khô… [4,5].…”