Enhanced Oral Bioavailability of The Antiretroviral Efavirenz Encapsulated in Poly(Epsilon-Caprolactone) Nanoparticles by A Spray-Drying Method

Abstract

EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance. Original submitted 2 May 2013; Revised submitted 4 September 2013.

Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

“…Spray-drying complies with both [38,39]. Moreover, when spray-drying is compared to other drying processes commonly used in industry such as freeze-drying, it is shorter and cheaper because it does not involve deep cooling, usually associated with great energy consumption [32,[40][41][42][43].…”

“…When these NPs were orally administered to rats, the AUC of the drug was about 9-fold higher than the one of the commercial product [126]. The change from a crystalline to an amorphous form also stresses the potential of spray-drying to produce pure drug NPs [39].…”

“…At the same time, it has increasingly attracted the interest of researchers to encapsulate drugs, extracts, aromatic oils, pigments, and flavors within different types of carriers such as polymeric nanoparticles (NPs) and microparticles (MPs) and nanocomposite MPs [42,43,52]. In addition, spray-drying is a processing method with great inherent potential to produce pure drug particles [39]. …”

Efavirenz Self-Nano-Emulsifying Drug Delivery System: In Vitro and In Vivo Evaluation

“…Major hurdles in poor therapeutic applications of this BCS class II drug are poor aqueous solubility (4 μg/mL), low intrinsic dissolution rate (0.037 mg/cm 2 /min), poor oral bioavailability (40-50%), and high protein-binding value (>99%) (14,15). Few attempts including bi-continuous nano-structured liquid crystalline particles (16), solid dispersions (17), spray drying (18), hot melt extrusion (19), co-micronization (20), and selfmicroemulsifying drug delivery systems (SMEDDS) (21,22) have been reported for improvement of solubility, bioavailability, dissolution profile, and physical stability EFV. Mean particle size of prepared liquid EFV-SMEDDS was approximately around 80 nm, and it does not exhibit satisfactory drug release at the end of 1 h. Still, no SNEDDS approach for the improvement of solubility and dissolution profile of EFV has been reported.…”

Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability

“…transformation of a material from a fluid state into a fine powder of solid dry particles with relatively narrow size distribution by atomization through a nozzle into a hot drying gas medium [25][26][27][28]. An additional appeal of this method is that enables the encapsulation of hydrophilic and hydrophobic drugs within polymeric particles [29][30][31] in relatively short time, without substantial thermal degradation (even of temperature-sensitive products) and with relatively high efficiency and yield [28,32].…”