Nanocrystalization: An Emerging Technology to Enhance the Bioavailability of Poorly Soluble Drugs

Abstract

Most of the active pharmaceutical ingredient used in the management of disease have poor water solubility and offer grueling problems in drug formulation development since low solubility is generally associated with poor dissolution characteristics which leads to poor oral bioavailability. The great challenge for the development of a pharmaceutical product is to create its new formulation and drug delivery system to limit solubility problems of existing drug candidate. Limited drug-loading capacity requires a large amount of carrier material to get appropriate encapsulation of the drug, which is another major challenge in the development of pharmaceutical product which could be resolved by developing nanocrystals (NCs). A significant research in the past few years has been done to develop NCs which helps in the delivery of poorly water soluble drugs via different routes. The technology could continue to thrive as a useful tool in pharmaceutical sciences for the improvement of drug solubility, absorption and bioavailability. Many crystalline compounds have pulled in incredible consideration much of the time, due to their ability to show good physical and chemical properties when contrasted with their amorphous counterparts. Nanocrystals have been proven to show atypical properties compared to the bulk. This review article explores the principles of the important nanocrystallization techniques including NCs characterization and its application.

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The Current Landscape of Novel Formulations and the Role of Mathematical Modeling in Their Development

“…They provide an excellent opportunity in the administration of hydrophobic drugs, which cannot be encapsulated well in liposomes and often have poor solubility and bioavailability when administered without nanoformulation. 30 Nanocrystalization increases the surface area-to-volume ratio, improves dissolution rates, and enhances solubility of hydrophobic drugs. A number of nanocrystal drug products have been approved for medical use with oral dosing, for a range of indications including for the treatment of pain, inflammation, hypercholesterolemia, and immunosuppression.…”

“…Instead of acting as a delivery system, encapsulating an active compound, the material itself is the active compound. They provide an excellent opportunity in the administration of hydrophobic drugs, which cannot be encapsulated well in liposomes and often have poor solubility and bioavailability when administered without nanoformulation 30 . Nanocrystalization increases the surface area‐to‐volume ratio, improves dissolution rates, and enhances solubility of hydrophobic drugs.…”

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“…The bioavailability of drugs depends on drugs' physiochemical and biological properties and the different ingredients used in their formulations for safe drug delivery system to targeted sites [5,8,9]. So, the development of safe drug delivery systems for a therapeutic agent with less side effects and more bioavailability to the targeted site is very vital in their formulation [10,11]. In order to overcome this situation innovative drug delivery systems are developing through colloidal drug carriers such as nanoparticles, microspheres, liposomes, polymer micelles [12].…”