Abstract
Solid drug nanoparticles (SDNs) are a nanotechnology with favourable characteristics to enhance drug delivery and improve the treatment of several diseases, showing benefit for improved oral bioavailability and injectable long‐acting medicines. The physicochemical properties and composition of nanoformulations can influence the absorption, distribution, and elimination of nanoparticles; consequently, the development of nanoparticles for drug delivery should consider the potential role of nanoparticle characteristics in the definition of pharmacokinetics. The aim of this study was to investigate the pharmacological behaviour of efavirenz SDNs and the identification of optimal nanoparticle properties and composition. Seventy‐seven efavirenz SDNs were included in the analysis. Cellular accumulation was evaluated in HepG2 (hepatic) and Caco‐2 (intestinal), CEM (lymphocyte), THP1 (monocyte), and A‐THP1 (macrophage) cell lines. Apparent intestinal permeability (Papp) was measured using a monolayer of Caco‐2 cells. The Papp values were used to evaluate the potential benefit on pharmacokinetics using a physiologically based pharmacokinetic model. The generated SDNs had an enhanced intestinal permeability and accumulation in different cell lines compared to the traditional formulation of efavirenz. Nanoparticle size and excipient choice influenced efavirenz apparent permeability and cellular accumulation, and this appeared to be cell line dependent. These findings represent a valuable platform for the design of SDNs, giving an empirical background for the selection of optimal nanoparticle characteristics and composition. Understanding how nanoparticle components and physicochemical properties influence pharmacological patterns will enable the rational design of SDNs with desirable pharmacokinetics.
Highlights
Efficacy and safety of therapies are influenced by the distribution of active pharmaceutical ingredients (APIs) into tissues and organs
A total of 77 efavirenz SDNs were included in the analysis
This study focused on the investigation of the pharmacological behaviour of efavirenz SDNs and the 2016 | Volume 1 | Issue 3 | Page 118
Summary
Efficacy and safety of therapies are influenced by the distribution of active pharmaceutical ingredients (APIs) into tissues and organs. The pharmacokinetics of APIs can be complicated by several processes such as poor absorption, low penetration in target tissues, and high metabolism and elimination rates. Nanoformulations have been applied to tackle these issues and enhance the delivery of APIs, exploiting the specific and unique properties of sub-micron particles. A broad spectrum of nanomedicine platforms for drug delivery has been developed using different technologies for improving pharmacokinetics, or active and passive targeting. APIs can be loaded into nanocarriers (e.g. liposomes, nanoemulsions, polymeric nanoparticles) to prevent chemical or enzymatic degradation and mediate enhanced penetration into cells, tissues, and organs (Marrache et al, 2013). Drugs can be linked to different inorganic nanoparticles, such as gold (Thakor et al, 2011), silver (Ong et al, 2013), silica (Wu et al, 2013), and iron (Ittrich et al, 2013)
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