Thermoresponsive gels containing gold nanoparticles (AuNPs) were prepared using Pluronic®127 alone (F1) and with hydroxypropyl methylcellulose (F2) at ratios of 15% w/w and 15:1% w/w, respectively. AuNPs were evaluated for particle size, zeta-potential, polydispersity index (PDI), morphology and XRD pattern. AuNP-containing thermoresponsive gels were investigated for their gelation temperature, gel strength, bio-adhesive force, viscosity, drug content, in vitro release and ex-vivo permeation, in addition to in vitro antibacterial activity against bacteria found in burn infections, Staphylococcus aureus. In vivo burn healing and antibacterial activities were also investigated and compared with those of a commercial product using burn-induced infected wounds in mice. Spherical AuNPs sized 28.9–37.65 nm displayed a surface plasmon resonance band at 522 nm, a PDI of 0.461, and a zeta potential of 34.8 mV with a negative surface charge. F1 and F2 showed gelation temperatures of 37.2 °C and 32.3 °C, bio-adhesive forces of 2.45 ± 0.52 and 4.76 ± 0.84 dyne/cm², viscosities of 10,165 ± 1.54 and 14,213 ± 2.31 cP, and gel strengths between 7.4 and 10.3 sec, respectively. The in vitro release values of F1 and F2 were 100% and 98.03% after 6 h, with permeation flux values of (J₁) 0.2974 ± 2.85 and (J₂) 0.2649 ± 1.43 (µg/cm²·h), respectively. The formulations showed antibacterial activity with the highest values for wound healing properties, as shown in vivo and by histopathological studies. This study demonstrates that a smart AuNPs thermoresponsive gel was successful as an antibacterial and wound healing transdermal drug delivery system.

The aim of this study is to prepare and evaluate the antibacterial and antibiofilm activity of ciprofloxacin (CIP) loaded PLGA nanoparticles (F2) and CIP-PLGA nanoparticles coated with chitosan (F3) versus ciprofloxacin solution (Fl) as a control on Enterococcus faecalis. F2 was prepared using double emulsion evaporation technique then coated with chitosan (F3). The prepared F2 and F3 were evaluated for size, surface charge, encapsulation efficiency, morphology and in vitro release. F1, F2, F3, and Chitosan (CS) were assessed in vitro using agar diffusion technique and biofilm inhibition assay. Finally, biofilm inhibition on teeth using Colony Forming Unit (CFU) was implemented with different concentrations of the three formulae. The results revealed that F2 is 202.9 nm with a negative charge −0.0254 mv, while F3 is 339.6 nm with a positive charge +28.5 mv. The encapsulation efficiency of F2, and F3 was 64% and 78% respectively. The amount released was 92.62% and 78.3% for F2 and F3, respectively, after 72 h, while F1 showed 100% released in the first hour. CS, F1, F2, and F3, showed antibacterial effect with inhibition zone of 12 mm, 22 mm, 20 mm, and 32 mm respectively. Biofilm inhibition of F1, F2, and F3 were 60%, 74%, and 91.8%, respectively. F3 colony count was less than F2, and F1 in all concentrations. It can be concluded that F3 had proven to exhibit potential antibacterial and antibiofilm activity in a controlled release pattern consequently, they can be used as an intra-canal medication.

Oromuco-adhesive films for buccal delivery of Propolis extract (PPE) entrapped in niosomes, were prepared to treat oral recurrent aphthous ulcer (RAU). PPE was investigated for antimicrobial compounds. Niosomes composed of span60 and cholesterol were evaluated for particles size, polydispersity index (PDI), zeta-potential, entrapment efficiency and in vitro release. The formed oromuco-adhesive films containing niosomal PPE were evaluated for swelling, mucoadhesion and elasticity. 24 patients suffering from RAU were divided equally into medicated and placebo groups and participated in this study to examine the onset of ulcer size reduction, complete healing and pain relief. Ultra-performance liquid chromatography-high resolution mass spectrometry revealed the presence of pinocembrin, pinobanksin, chrysin and galangin as antimicrobial flavonoids with total content of 158.7 ± 0.15 µg quercetin equivalents and phenolic content of 180.8 ± 0.11 µg gallic acid equivalents/mg. Multilamellar niosomes of 176–333 nm displayed entrapment efficiency of 91 ± 0.48%, PDI of 0.676 and zeta potential of −4.99. In vitro release after 8 h from niosomal dispersion and films were 64.05% and 29.09 ± 0.13% respectively. Clinical results revealed duration of film adherence from 2–4 h in the two groups. The onset of ulcer size reduction in medicated group was attained within second and third day, complete healing was achieved within first 10 days of treatment and pain relief lasted for more than 4–5 h, in contrast to the placebo group. This oromuco-adhesive films which offer controlled and targeting drug delivery can be proposed as a new therapeutic strategy in the treatment of oral recurrent aphthous ulcer.

Niosomes entrapping pregabalin (PG) were prepared using span 60 and cholesterol in different molar ratios by hydration method, the remaining PG from the hydrating solution was separated from vesicles by freeze centrifugation. Optimization of nano-based carrier of pregabalin (PG) was achieved. Quality by Design strategy was successfully employed to obtain PG-loaded niosomes with the desired properties. The optimal particle size, drug release and entrapment efficiency were attained by Minitab^® program using design of experiment (DOE) that predicted the best parameters by investigating the combined effect of different factors simultaneously. Pareto chart was used in the screening step to exclude the insignificant variables while response surface methodology (RSM) was used in the optimization step to study the significant factors. Best formula was selected to prepare topical hydrogels loaded with niosomal PG using HPMC and Carbopol 934. It was verified, by means of mechanical and rheological tests, that addition of the vesicles to the gel matrix affected significantly gel network. In vitro release and ex vivo permeation experiments were carried out. Delivery of PG molecules followed a Higuchi, non Fickian diffusion. The present work will be of interest for pharmaceutical industry as a controlled transdermal alternative to the conventional oral route.

Background: Atorvastatin calcium (AT) is an ocular anti-inflammatory with limited bioavailability when taken orally due to its low solubility in low pH and extensive first-pass effect. To overcome these problems, AT was entrapped in polymeric nanoparticles (NPs) to improve surface properties and sustained release, in addition to achieving site-specific action. Methods: AT was entrapped in chitosan (CS)-coated polylactic-co-glycolic acid (PLGA) NPs to form AT-PLGA-CS-NPs (F1). F1 and free AT were embedded in thermosensitive Pluronic^® 127-hydroxypropyl methylcellulose (HPMC) to form thermosensitive gels (F2) and (F3) while F4 is AT suspension in water. F1 was assessed for size, surface charge, polydispersity index (PDI), and morphology. F2 and F3 were examined for gelation temperature, gel strength, pH, and viscosity. In vitro release of the four formulations was also investigated. The ocular irritancy and anti-inflammatory efficacy of formulations against prostaglandin E₁-(PGE₁) induced ocular inflammation in rabbits were investigated by counting the polymorphonuclear leukocytes (PMNs) and protein migrated in tears. Results: Oval F1 of 80.0– 190.0± 21.6 nm exhibited a PDI of 0.331 and zeta potential of ‏ 17.4± 5.62 mV with a positive surface charge. F2 and F3 gelation temperatures were 35.17± 0.22°C and 36.93± 0.31°C, viscosity 12,243± 0.64 and 9759± 0.22 cP, gel strength 15.56± 0.6 and 12.45± 0.1 s, and pHs of 7.4± 0.02 and 7.4± 0.1, respectively. In vitro release of F1, F2, F3, and F4 were 48.21± 0.31, 26.48± 0.5, 84.76± 0.11, and 100% after 24 hrs, respectively. All formulations were non-irritant. F2 significantly inhibited lid closure up to 3 h, PMN counts and proteins in tear fluids up to 5 h compared to other formulations. Conclusion: AT-PLGA-CS-NP thermosensitive gels proved to be successful ocular anti-inflammatory drug delivery systems.