Chitosan Nanocarrier Entrapping Hydrophilic Drugs as Advanced Polymeric System for Dual Pharmaceutical and Cosmeceutical Application: A Comprehensive Analysis Using Box-Behnken Design

The objective of the present research is to propose chitosan as a nanocarrier for caffeine—a commonly used drug in combating cellulite. Being a hydrophilic drug, caffeine suffers from insufficient topical penetration upon application on the skin. Chitosan nanoparticles loaded with caffeine were prepared via the ionic gelation technique and optimized according to a Box–Behnken design. The effect of (A) chitosan concentration, (B) chitosan solution pH, and (C) chitosan to sodium tripolyphosphate mass ratio on (Y1) entrapment efficiency percent, (Y2) particle size, (Y3) polydispersity index, and (Y4) zeta potential were studied. Subsequently, the desired constraints on responses were applied, and validation of the optimization procedure was confirmed by the parameters exhibited by the optimal formulation. A caffeine entrapment efficiency percent of 17.25 ± 1.48%, a particle size of 173.03 ± 4.32 nm, a polydispersity index of 0.278 ± 0.01, and a surface charge of 41.7 ± 3.0 mV were attained. Microscopical evaluation using transmission electron microscope revealed a typical spherical nature of the nanoparticles arranged in a network with a further confirmation of the formation of particles in the nano range. The results proved the successful implementation of the Box–Behnken design for optimization of chitosan-based nanoparticles in the field of advanced polymeric systems for pharmaceutical and cosmeceutical applications

Enhancement of dissolution and oral bioavailability of lacidipine via pluronic P123/F127 mixed polymeric micelles: formulation, optimization using central composite design and in vivo bioavailability study

This study aims at preparing and optimizing lacidipine (LCDP) polymeric micelles using thin film hydration technique in order to overcome LCDP solubility-limited oral bioavailability. A two-factor three-level central composite face-centered design (CCFD) was employed to optimize the formulation variables to obtain LCDP polymeric micelles of high entrapment efficiency and small and uniform particle size (PS). Formulation variables were: Pluronic to drug ratio (A) and Pluronic P123 percentage (B). LCDP polymeric micelles were assessed for entrapment efficiency (EE%), PS and polydispersity index (PDI). The formula with the highest desirability (0.959) was chosen as the optimized formula. The values of the formulation variables (A and B) in the optimized polymeric micelles formula were 45% and 80%, respectively. Optimum LCDP polymeric micelles had entrapment efficiency of 99.23%, PS of 21.08 nm and PDI of 0.11. Optimum LCDP polymeric micelles formula was physically characterized using transmission electron microscopy. LCDP polymeric micelles showed saturation solubility approximately 450 times that of raw LCDP in addition to significantly enhanced dissolution rate. Bioavailability study of optimum LCDP polymeric micelles formula in rabbits revealed a 6.85-fold increase in LCDP bioavailability compared to LCDP oral suspension

Different Curcumin-Loaded Delivery Systems for Wound Healing Applications: A Comprehensive Review

Curcumin or turmeric is the active constituent of Curcuma longa L. It has marvelous medicinal applications in many diseases. When the skin integrity is compromised due to either acute or chronic wounds, the body initiates several steps leading to tissue healing and skin barrier function restoration. Curcumin has very strong antibacterial and antifungal activities with powerful wound healing ability owing to its antioxidant activity. Nevertheless, its poor oral bioavailability, low water solubility and rapid metabolism limit its medical use. Tailoring suitable drug delivery systems for carrying curcumin improves its pharmaceutical and pharmacological effects. This review summarizes the most recent reported curcumin-loaded delivery systems for wound healing purposes, chiefly hydrogels, films, wafers, and sponges. In addition, curcumin nanoformulations such as nanohydrogels, nanoparticles and nanofibers are also presented, which offer better solubility, bioavailability, and sustained release to augment curcumin wound healing effects through stimulating the different healing phases by the aid of the small carrier

Transdermal Delivery of an Anti-Cancer Drug via W/O Emulsions Based on Alkyl Polyglycosides and Lecithin: Design, Characterization, and In Vivo Evaluation of the Possible Irritation Potential in Rats

The purpose of this work was to develop w/o emulsions that could be safely used to promote transdermal delivery of 5-fluorouracil (5-FU). Two pseudo-ternary phase diagrams comprising oleoyl-macrogol glycerides, water, and a surfactant/co-surfactant (S/CoS) mixture of lecithin, ethanol, and either coco glucoside or decyl glucoside were investigated for their potential to develop promising 5-FU emulsions. Six systems were selected and subjected to thermodynamic stability tests; heat–cool cycles, centrifugation, and finally freeze–thaw cycles. All systems passed the challenges and were characterized for transmission electron microscopy, droplet size, rheological behavior, pH, and transdermal permeation through newly born mice skin in Franz diffusion cells. The systems had spherical droplets ranging in diameter from 1.81 to 2.97 μm, pH values ranging from 7.50 to 8.49 and possessed Newtonian flow. A significant (P < 0.05) increase in 5-FU permeability parameters as steady-state flux, permeability coefficient was achieved with formula B5 comprising water (5% w/w), S/CoS mixture of lecithin/ethanol/decyl glucoside (14.67:12.15:18.18% w/w, respectively) and oleoyl-macrogol glycerides (50% w/w). When applied to shaved rat skin, this system was well tolerated with only moderate skin irritation that was recovered within 12 h. Indeed, minor histopathologic changes were observed after 5-day treatment. Further studies should be carried out, in the future, to investigate the potentiality of this promising system to promote transdermal delivery of 5-FU through human skin