Nanoencapsulation of Drugs
It is well known that water insoluble or poorly soluble drugs are extremely difficult to formulate. Their incompatibility with water-based physiological environments such as blood, cytoplasm, and other bodily fluids present a major challenge in delivery, biodistribution, and bioavailability.
Nanoencapsulation can improve the solubility and pharmacokinetic profiles of such insoluble drugs. In many cases, targeted drug delivery is greatly enhanced, bioavailability to the target tissues and cells are significantly improved, while toxicity is reduced. In various cases involving insoluble anti-cancer drugs, the ANP team has successfully demonstrated that nanoencapsulation can significantly enhance the delivery of such drugs to tumor tissue and minimize their toxic side effects to normal cells.
On the other hand, hydrophilic small molecule drugs often suffer from rapid blood clearance, poor membrane transport properties, and sometimes poor in vivo stability. Nanoencapsulation of these soluble drugs has been shown to improve trans-membrane delivery to afflicted cells. In addition, the half-lives of these drugs in blood circulation have been significantly increased by encapsulation, reducing multiple dosing and minimizing side effects.
Many biologic drugs such as therapeutic peptides and recombinant proteins tend to form aggregates during formulation and in vivo delivery due to protein folding and/or localized charge interactions. Such aggregations may cause severe immunogenic responses. In addition, these biologic drugs often exhibit a short PK profile. Nanoencapsulation of these biotherapeutics greatly improves their PK profile in vivo, similar to PEGylated proteins, while preventing the undesired aggregates from forming. Nanoencapsulation has also been demonstrated to preserve and protect the optimal three dimensional configuration of these complex molecules so that bioactive proteins such as enzymes exhibit higher specific activity when nanoencapsulated.