Oral Treatment of Spontaneously Hypertensive Rats with Captopril-Surface Functionalized Furosemide-Loaded Multi-Wall Lipid-Core Nanocapsules.

Multi-wall lipid-core nanocapsule (MLNC) functionalized with captopril and nanoencapsulating furosemide within the core was developed as a liquid formulation for oral administration. The nanocapsules had mean particle size below 200 nm, showing unimodal and narrow size distributions with moderate dispersity (laser diffraction and dynamic light scattering). Zeta potential was inverted from -14.3 mV [LNC-Fur(0,5)] to +18.3 mV after chitosan coating. Transmission electron microscopy and atomic force microscopy showed spherical structures corroborating the nanometric diameter of the nanocapsules. Regarding the systolic pressure, on the first day, the formulations showed antihypertensive effect and a longer effect than the respective drug solutions. When both drugs were associated, the anti-hypertensive effect was prolonged. On the fifth day, a time effect reduction was observed for all treatments, except for the nanocapsule formulation containing both drugs [Capt(0.5)-Zn(25)-MLNC-Fur(0.45)]. For diastolic pressure, only Capt(0.5)-Zn(25)-MLNC-Fur(0.45) presented a significant difference (p < 0.05) on the first day. On the fifth day, both Capt(0.5)-MLNC-Fur(0.45) and Capt(0.5)-Zn(25)-MLNC-Fur(0.45) had an effect lasting up to 24 h. The analysis of early kidney damage marker showed a potential protection in renal function by Capt(0.5)-Zn(25)-MLNC-Fur(0.45). In conclusion, the formulation Capt(0.5)-Zn(25)-MLNC-Fur(0.45) proved to be suitable for hypertension treatment envisaging an important innovation.

Development of an Insect Repellent Spray for Textile Based on Permethrin-Loaded Lipid-Core Nanocapsules.

The aim of this study was to prepare and characterize permethrin-loaded lipid core nanocapsules (P-LNC) in order to produce a long last insect repellent spray formulation for clothes. P-LNC were prepared by self-assembling in aqueous solution showing a mean diameter of 201 +/- 4 nm with a monomodal distribution, a permethrin content of 4.6 +/- 0.1 mg/mL and zeta potential of--16.7 +/- 4 mV. P-LNC (0.46%), as well as the commercial product (0.46%) and the hydroalcoholic solution (0.50%) of permethrin were separately sprayed onto cotton or polyester, followed by successive washes of the fabric. The results showed that the fabrics treated with P-LNC are more resistant than other solutions in terms of remaining permethrin content. After twenty washes, the cotton treated with P-LNC, presented a concentration of 566 +/- 27 mg/M2 of impregnated permethrin, while for the treatment with the substance hydroalcoholic solution and with the commercial product the concentrations values were of 340 +/- 7 mg/M2 and 224 +/- 74 mg/M2, respectively. When the test was performed using polyester, this fiber was less adhesive than cotton, resulting in a final concentration of permethrin (after 20 washes) of 81 +/- 10 mg/m2 for P-LNC suspension, 94 +/- 8 mg/M2 for the substance hydroalcoolic solution and 22 +/- 3 mg/M2 for the commercial product. After impregnating cotton with the formulations and submitting to a temperature of 200 degrees C, the P-LNC also demonstrated higher adherence compared to the other formulations (407 +/- 67 mg/m2 for P-LNC, 236 +/- 72 mg/m2 for the substance hydroalcoholic solution and 158 +/- 62 mg/m2 for commercial product). These results showed that the repellent spray composed of P-LNC developed in this work is a promising and innovative product for the individual protection against insects, useful for impregnation onto cotton garments.

Hydrogel containing adapalene- and dapsone-loaded lipid-core nanocapsules for cutaneous application: development, characterization, in vitro irritation and permeation studies.

Lipid-core polymeric nanocapsule suspensions containing adapalene and dapsone (AD-LCNC) were developed and incorporated in a Carbopol 940® hydrogel (AD-LCNC HG). A nanoemulsion (AD-NE), similarly prepared but omitting the polymer, was developed and also incorporated in a Carbopol 940® hydrogel (AD-NE HG) to evaluate the polymer effect. Physicochemical characteristics were evaluated. AD-LCNC suspensions containing 0.07% of dapsone and 0.025% of adapalene presented an average size of 194.9 ± 0.42 nm, zeta potential of -15 ± 1.2 mV and polydispersity index of 0.12 ± 0.02, using electrophoretic light scattering (n = 3). The granulometric profiles showed unimodal size distributions for AD-LCNC suspensions, demonstrating that no microscopic population is present in the formulation. No instability phenomena were observed by multiple light-scattering analysis. Photomicrographs obtained by TEM showed homogeneous- and spherical-shaped particles. The encapsulation efficiency was 99.99% for dapsone and 100% for adapalene. The pH values for AD-LCNC suspensions were 5.1 and 7.6 for AD-LCNC HG. Formulations were classified as nonirritant in the HET-CAM test. Rheological analysis demonstrated a non-Newtonian pseudoplastic profile. The in vitro skin permeation studies showed a higher amount of adapalene in epidermis (130.52 ± 25.72 ng/mg) and dermis (4.66 ± 2.5 ng/mg) for AD-NE HG. The AD-LCNC HG presented higher amount of dapsone in both the skin layers (73.91 ± 21.64 ng/mg in epidermis and 4.08 ± 0.85 ng/mg in dermis). The assay showed significant difference between AD-LCNC HG and AD-NE HG (p < 0.05), and drug was not found in the receptor medium.