Abstract
The purpose of this work was to more exhaustively study the influence of nanocarrier matrix composition and also the polyethylene glycol (PEG)-modified surface on the performances of formulations as lipophilic drug delivery systems. Poly (d,l-lactide-co-glycolide), two vegetable oils (Nigella sativa oil and Echium oil) and indomethacin were employed to prepare novel PEG-coated nanocarriers through emulsion solvent evaporation method. The surface modification was achieved by physical PEG adsorption (in the post-production step). Transmission electron microscopy (TEM) nanographs highlighted the core-shell structure of hybrid formulations while scanning electron microscopy (SEM) images showed no obvious morphological changes after PEG adsorption. Drug loading (DL) and entrapment efficiency (EE) varied from 4.6% to 16.4% and 28.7% to 61.4%, solely depending on the type of polymeric matrix. The oil dispersion within hybrid matrix determined a more amorphous structure, as was emphasized by differential scanning calorimetry (DSC) investigations. The release studies highlighted the oil effect upon the ability of nanocarrier to discharge in a more sustained manner the encapsulated drug. Among the kinetic models employed, the Weibull and Korsmeyer-Peppas models showed the better fit (R2 = 0.999 and 0.981) with n < 0.43 indicating a Fickian type release pattern. According to cytotoxic assessment the PEG presence on the surface increased the cellular viability with ~1.5 times as compared to uncoated formulations.
Highlights
The use of a suitable drug delivery system has become an important approach for emerging valuable therapy
The extensive apoptotic cell death and the substantial anti-tumorigenic effects of ATRA-PLGA-synthetic oil nanoparticles (PONC) (IC50 of ATRA-PONC: 2 μg/mL versus free ATRA: 17.5 μg/mL) in ovarian cancer cell subline SKOV-3PR were owed to higher cell permeation by the well-dispersed drug/oil gradually released from PONC [3,4]
The following IMC-loaded nanocarriers were prepared: PLGA-IMC (IMC encapsulated into PLGA standard nanoparticles without surface modification), HPON-IMC (IMC incorporated into hybrid nanoparticles containing 1/1 wt PLGA/Nigella sativa oil (NSO) ratio), and HPOE-IMC (IMC loaded into hybrid nanoparticles containing 1/0.5 wt PLGA/EQ ratio); as well as PLGA-IMC-polyethylene glycol (PEG), HPON-IMC-PEG, and HPOE-IMC-PEG (IMC-loaded into standard or hybrid systems coated with PEG)
Summary
The use of a suitable drug delivery system has become an important approach for emerging valuable therapy. The hybridization process of poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles is one of the most promising tools for improving their efficacy in drug delivery applications [1]. The concept of hybrid formulations which result by physical association of PLGA nanoparticles and different vegetable/synthetic oils is a new trend in obtaining versatile carriers. The authors reported a higher encapsulation efficiency of ATRA into hybrid nanocarriers and more sustained release profile, avoiding the risk of uncontrolled initial burst release. These performances were attributed to the oil inclusion which introduced nanostructure into the polymeric matrix of the carrier. The extensive apoptotic cell death and the substantial anti-tumorigenic effects of ATRA-PONC (IC50 of ATRA-PONC: 2 μg/mL versus free ATRA: 17.5 μg/mL) in ovarian cancer cell subline SKOV-3PR were owed to higher cell permeation by the well-dispersed drug/oil gradually released from PONC [3,4]
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