Synthesis and characterization of osmotic pump capsules containing polyoxyethylene and pH modifier to control the release of nifedipine.

The aim of this study was to formulate osmotic pump capsules (OPCs) to control the release of nifedipine (NP). NP solid dispersion was prepared by solvent evaporation method. The prepared mixture of NP solid dispersion and various excipients were filled into the commercial HPMC hard capsule shells and then coated with cellulose acetate (CA) solution to form NP-OPC. The CA coating solution consisted of CA as semi-permeable membrane, and Poloxamer 188 as pore formers. The impact of addition agents, citric acid and pore formers on in vitro drug release were investigated. Furthermore, the study has highlighted the impact of paddle speed and the pH value of release media, on the release and compared the release with the commercial controlled release tablets. The in vitro drug release study indicated that drug release could reach 95% in 24 h with optimal formulation, and interestingly model fitting showed that the drug release behavior was closely followed to zero-order release kinetics. The pharmacokinetic studies were performed in rabbits with commercial controlled release tablets as reference, both preparations showed a sustained release effect. Compared with traditional preparation methods of OPCs, the new preparation process was simplified without the operation of laser drilling and the sealing process of capsule body and cap, which improved the feasibility of industrial production.

Microfluidic Assembly: An Innovative Tool for the Encapsulation, Protection, and Controlled Release of Nutraceuticals.

Nutraceuticals have been gradually accepted as food ingredients that can offer health benefits and provide protection against several diseases. It is widely accepted due to potential nutritional benefits, safety, and therapeutic effects. Most nutraceuticals are vulnerable to the changes in the external environment, which leads to poor physical and chemical stability and absorption. Several researchers have designed various encapsulation technologies to promote the use of nutraceuticals. Microfluidic technology is an emerging approach which can be used for nutraceutical delivery with precise control. The delivery systems using microfluidic technology have obtained much interest in recent years. In this review article, we have summarized the recently introduced nutraceutical delivery platforms including emulsions, liposomes, microspheres, microgels, and polymer nanoparticles based on microfluidic techniques. Emphasis has been made to discuss the advantages, preparations, characterizations, and applications of nutraceutical delivery systems. Finally, the challenges, several up-scaling methods, and future expectations are discussed.

Nanoemulsion-based delivery approaches for nutraceuticals: fabrication, application, characterization, biological fate, potential toxicity and future trends.

In the modern food industry, people are paying more and more attention to the use of edible nanoemulsions to encapsulate, protect and deliver lipophilic functional ingredients, such as volatile additives, polyphenols, aromas, pigments, proteins, vitamins, oil-soluble flavors, preservatives, etc., which are the current global needs. Nanoemulsions are constructed with droplets of nano range size and they offer many potential advantages over conventional emulsions including the delivery of both hydrophilic and hydrophobic compounds, higher stability, better antibacterial properties, good taste experience, higher affinity, longer shelf-life and improvement of the bioavailability of components. Moreover, they are highly capable of improving the wettability and/or solubility of poorly water-soluble compounds, which may result in better pharmacokinetic and pharmacodynamic properties of nutraceutical compounds. On the other hand, oral nanoemulsions also have certain risks, such as their ability to change the biological fate of biologically active ingredients in the gastrointestinal tract and the potential toxicity of certain ingredients used in their production. This review article summarizes the manufacturing, application, characterization, biological fate, potential toxicity, and future challenges and trends of nanoemulsions, and focuses on nanoemulsion-based nutraceutical delivery approaches suitable for the food industry.

An overview of preparation and evaluation sustained-release injectable microspheres.

Recently, sustained-release injectable microspheres as a novel parenteral administration system have been interested on for many years, due to the excellent advantages when compared to traditional dosage forms: less administration frequency, lower adverse side effects and no need for a surgical procedure. Therefore, major progresses in the development of another successful marketed sustained-release injectable formation have been made, but most investigations are merely limited in laboratory levels; in addition, few reports focus on giving some positive guidance to launch these novel microspheres into market. This review addressed some commonly used polymers, preparation methods and sterilization processes relating to biodegradable microspheres. Moreover, the processes for measuring the sustained-release behaviour of this novel system are summarized in this report, including the methods to determine the in vitro and in vivo release behaviours and the strategies to analyse the in vitro and in vivo correlations.

Increase of therapeutic activity of doxorubicin by long circulating liposomes in combination with curcumin.

In this study, doxorubicin (DOX)-loaded long circulating liposomes combined with curcumin (CUR) (DOX-CUR-LCLs) were successfully prepared as a novel formulation for cancer treatment. The particle size and distribution, zeta potential, drug loading capacity, and entrapment efficiency (EE) of the preparation were characterized. The in vitro anti-tumor activities of DOX-CUR-LCLs and DOX-LCLs against A549 cells were then evaluated and compared with that of free DOX. Cytotoxicity evaluation showed that DOX-CUR-LCLs had a significantly higher antitumor activity than other DOX preparations. These results suggest that novel DOX-CUR-LCLs, combination of DOX and CUR administered in long-circulating liposomes, could improve antitumor activity.

Preparation and enhanced oral bioavailability of cryptotanshinone-loaded solid lipid nanoparticles.

In this study, solid lipid nanoparticles (SLNs) were successfully prepared by an ultrasonic and high-pressure homogenization method to improve the oral bioavailability of the poorly water-soluble drug cryptotanshinone (CTS). The particle size and distribution, drug loading capacity, drug entrapment efficiency, zeta potential, and long-term physical stability of the SLNs were characterized in detail. A pharmacokinetic study was conducted in rats after oral administration of CTS in different SLNs, and it was found that the relative bioavailability of CTS in the SLNs was significantly increased compared with that of a CTS-suspension. The incorporation of CTS in SLNs also markedly changes the metabolism behavior of CTS to tanshinone IIA. These results indicate that CTS absorption is enhanced significantly by employing SLN formulations, and SLNs represent a powerful approach for improving the oral absorption of poorly soluble drugs.