Sustained Release from Lipid-Core Nanocapsules by Varying the Core Viscosity and the Particle Surface Area

Abstract

Based on the structure of polymeric nanocapsules containing a lipid-dispersed core composed of caprylic/capric trygliceride (CCT) and sorbitan monostearate (SM), we hypothesized that varying the core component concentrations the drug release kinetic could be modulated. Our objective was also to determine the parameters which were responsible for controlling the drug release kinetics. The nanocapsules were prepared by interfacial deposition of poly(epsilon-caprolactone). Interfacial hydrolysis of indomethacin ester (IndOEt) was used to simulate a sink condition of release. Mathematical modeling showed that the IndOEt half-lives increased (198 to 378 and 263 to 508 min) with the increase in the core lipid concentrations, and that the release mechanism was the anomalous transport. By increasing the SM concentration, the diameters were constant (around 250 nm) and the surface areas increased (from 1 06 × 10 4 to 1 51 × 10 4 cm 2 · ml −1 ), while by increasing the CCT concentration, the diameters increased (215 to 391 nm) and the surface areas reduced (1 46 × 10 4 to 1 06 × 10 4 cm 2 · ml −1 ). The presence of SM increased the viscosity of CCT and the IndOEt apparent permeability decreased from 4 26 × 10 −7 to 2 54 × 10 −7 cm · s −1 , while for CCT series, the apparent permeability was constant around 3 0 × 10 −7 cm · s −1 . A mathematical correlation was established and the IndOEt apparent permeability can be estimated by the SM concentration. In conclusion, varying the CCT and SM concentrations the IndOEt release was controlled by the nanocapsule surface area and by the viscosity of the core, respectively.

Nanocarriers for optimizing the balance between interfollicular permeation and follicular uptake of topically applied clobetasol to minimize adverse effects

“…For the preparation of NS the organic phase contained only PCL and sorbitan monostearate. For NC capric/caprylic triglycerides (CCT) was added as a liquid lipid core, and LNC contained PCL, CCT and the lipophilic surfactant sorbitan monostearate dispersed in the core forming an organogel [25]. In contrast to NS (matricial system), both NC and LNC gave rise to a core and shell structure.…”

Vegetable oils as core of cationic polymeric nanocapsules: influence on the physicochemical properties

“…Among them, the nanocapsules differ by the presence of an oily core that can act as reservoir for lipophilic drugs [4,5]. The choice of the oily core is important for the control of the drug release [6] and the particle stability since some core components are capable of dissolving the polymer network [7]. Similar to the vegetable oils, the nanoparticles present a great applicability in cosmetics or dermatological products [8].…”

Validation of analytical method by HPLC for determination of dapsone in polymeric nanocapsules based on crude rice brain oil

“…The nanocapsules were prepared by interfacial deposition method of the preformed polymer (Jager et al, 2009). The organic phase, consisting of acetone (30 mL), dapsone (0.01 g), PCL (0.1 g), sorbitan monostearate (0.077 g) and crude rice bran oil (0.15 g), was poured into the aqueous phase (50 mL) containing polysorbate 80 (0.077 g), under moderate magnetic stirring.…”