Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Several plant bioactive compounds have exhibited functional activities that suggest they could play a remarkable role in preventing a wide range of chronic diseases. The largest group of naturally-occurring polyphenols are the flavonoids, including apigenin. The present work is an updated overview of apigenin, focusing on its health-promoting effects/therapeutic functions and, in particular, results of in vivo research. In addition to an introduction to its chemistry, nutraceutical features have also been described. The main key findings from in vivo research, including animal models and human studies, are summarized. The beneficial indications are reported and discussed in detail, including effects in diabetes, amnesia and Alzheimer’s disease, depression and insomnia, cancer, etc. Finally, data on flavonoids from the main public databases are gathered to highlight the apigenin’s key role in dietary assessment and in the evaluation of a formulated diet, to determine exposure and to investigate its health effects in vivo.

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The Therapeutic Potential of Apigenin.

Spray drying formulation of amorphous solid dispersions.

Amorphous solid dispersions: Rational selection of a manufacturing process.

To overcome the shortcomings of conventional dosage forms, targeted and modified drug delivery system came into existence. This was the time when a novel drug delivery system was in high demand. Nanoparticles are such type of targeted drug delivery system. Nanoparticles are colloidal particles which provide site-specific delivery of drugs. There are different kinds of nanoparticles, polymeric nanoparticles are one of a kind. Polymeric nanoparticles, nowadays, is one of the most researched topics. Their major advantages include good control over size, longer clearance time, improved therapeutic efficacy and reduced toxicity. Polymer-based nanoparticles come in various forms like dendrimers, ligand-based nanoparticles, polymeric micelles, PEGylated nanoparticles, etc. This chapter includes the various advancements in polymeric nanoparticles as well as advancements in the polymers that are used in their preparation. It reveals details about functionalized nanoparticles and its types. It finally discusses the use of various polymers in the drug delivery system in order to target varied diseases, taking cancer and vaginal diseases as an example. The chapter at the end also reveals the future aspect of functionalized polymeric nanoparticles.

Recent developments in functionalized polymer nanoparticles for efficient drug delivery system

Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs.

New method and characterization of self-assembled gelatin-oleic nanoparticles using a desolvation method via carbodiimide/N-hydroxysuccinimide (EDC/NHS) reaction.

In this work, a novel, biocompatible conjugates of gelatin and oleic acid (GOC) were synthesized by a novel aqueous solvent-based method that overcame challenges of completely contrary solubility between gelatin and oleic acid (OA). The GO nanoparticles (GONs) and Paclitaxel encapsulated nanoparticles (PTX-GON) were prepared by self-assembly in water. These nanoparticles (NPs) were then conjugated with folic acid (FA) for targeting cervical cancer cells (Hela cells) and were characterized for their various physicochemical and pharmaceutical properties. Fourier transform infrared spectroscopy (FT-IR) and 1H NMR studies indicated the successful synthesis of GOC which showed low critical aggregation concentration in water (0.015 mg/ml). All NPs were stable in human blood serum and their mean diameters were below 300 nm suitable for passive targeting. Powder X-ray diffraction (PXRD) diffractograms showed the reduction in drug crystallinity and hence, leading to the solubility enhancement of PTX. The release of PTX from both PTX-GON and FA conjugated PTX-GON (PTX-FA-GON) was controlled for a long time. The cytotoxicity results demonstrated great advantages of PTX-FA-GON and PTX-GON over the conventional dosage form of pacliaxel (Taxol). These results, therefore, indicate that GOC is a promising material to prepare drug encapsulated NP as a controlled delivery system and PTX-FA-GON is a potential targeted delivery system for cancer therapy.

Chau Le-Ngoc Vo

Papers

Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs.

New method and characterization of self-assembled gelatin-oleic nanoparticles using a desolvation method via carbodiimide/N-hydroxysuccinimide (EDC/NHS) reaction.

Novel multifunctional biocompatible gelatin-oleic acid conjugate: self-assembled nanoparticles for drug delivery.

Electrostatically assembled wound dressings deliver pro-angiogenic anti-miRs preferentially to endothelial cells.