Semi-Solid Dosage Forms Containing Pranoprofen-Loaded NLC as Topical Therapy for Local Inflammation: In Vitro, Ex Vivo and In Vivo Evaluation

Abstract

Pranoprofen (PRA)-loaded nanostructured lipid carriers (NLC) have been dispersed into blank gels composed of 1% of Carbomer 940 (PRA-NLC-Car) and 3% of Sepigel® 305 (PRA-NLC-Sep) as a novel strategy to refine the biopharmaceutical profile of PRA, for dermal administration in the treatment of skin inflammation that may be caused by possible skin abrasion. This stratagem intends to improve the joining of PRA with the skin, improving its retention and anti-inflammatory effect. Gels were evaluated for various parameters such as pH, morphology, rheology, and swelling. In vitro drug release research and ex vivo permeation through the skin were carried out on Franz diffusion cells. Additionally, in vivo assays were carried out to evaluate the anti-inflammatory effect, and tolerance studies were performed in humans by evaluating the biomechanical properties. Results showed a rheological profile common of semi-solid pharmaceutical forms for dermal application, with sustained release up to 24 h. In vivo studies using PRA-NLC-Car and PRA-NLC-Sep in Mus musculus mice and hairless rats histologically demonstrated their efficacy in an inflammatory animal model study. No signs of skin irritation or modifications of the skin’s biophysical properties were identified and the gels were well tolerated. The results obtained from this investigation concluded that the developed semi-solid formulations represent a fitting drug delivery carrier for PRA’s transdermal delivery, enhancing its dermal retention and suggesting that they can be utilized as an interesting and effective topical treatment for local skin inflammation caused by a possible abrasion.

Topical Meloxicam Hydroxypropyl Guar Hydrogels Based on Low-Substituted Hydroxypropyl Cellulose Solid Dispersions

“…Furthermore, under a constant rate cycle of 50 s −1 , the mean viscosity values at 25 • C were 12.18 ± 0.26 Pa•s for H-Blank and 12.46 ± 0.42 Pa•s for HMX − RM, respectively. Similar increases at low shear rate values (50 s −1 ) have been previously observed in guar gum hydrogels loaded with different drugs, maintaining a decreased viscosity when the shear rate increases, which is a critical property for easy topical administration [37]. In addition, different studies indicated that the viscosity of the hydrogels played an important role in the percentage of drug release [6].…”

“…The viscosity results for these hydrogels with a constant shear rate of 50 s −1 were 9.22 ± 0.26, 12.18 ± 0.26, and 17.45 ± 0.28 Pa·s for blank HPG hydrogels with percentages of 1.0, 1.75 and 2.5%, respectively. These results showed that a gelling agent concentration of 1.75% ( w / v ) HPG produced a gel with adequate viscosity values, which would be suitable for topical administration [ 5 , 37 ]. This concentration was selected for further analysis: viscosity, FTIR, SEM, dissolution, and kinetic studies.…”

“…Similar slow dissolution profiles for poorly soluble drugs, such as MX, have been previously reported [ 21 ]. The delayed dissolution profile of hydrogels containing 1.75% HPG was related to its viscosity [ 6 , 37 ].…”

Electrosprayed Stearic-Acid-Coated Ethylcellulose Microparticles for an Improved Sustained Release of Anticancer Drug

“…Numerous reports in the literature have demonstrated that insoluble and biodegradable polymers and their composites and hybrids can be exploited as carriers to manipulate the gradual release of the loaded drug molecules [ 75 , 76 , 77 , 78 ]. Meanwhile, lipid materials are also frequently explored for the extended release of drugs in the formation of microparticles, micelles, composites, solid nanoparticles, emulsions, and liposome [ 79 , 80 , 81 , 82 , 83 ]. Thus, firstly, in this study, both insoluble polymer EC gels and the lipid SA were selected as the TC carrier, which are materials selected from experiences with the traditional pharmaceutics.…”

Natural-Origin Betaine Surfactants as Promising Components for the Stabilization of Lipid Carriers

“…Among the ways of application of colloidal systems based on solid lipids extensively documented in the literature are cosmetic [5,8,9], food [4,6,10], and, above all, in the pharmaceutical industry (i.e., drug delivery) [7,11,12]. In recent years, lipid formulations have enabled the effective encapsulation of active substances successfully delivered intravenously [13][14][15], orally [16][17][18], transdermally [19][20][21], and also directly into the eye [22][23][24] or nose [25][26][27].…”