Enhanced antibacterial and genoprotective properties of nanoliposomal Satureja hortensis L. essential oil.

Nanoliposomes are drug delivery systems that improve bioavailability by encapsulating therapeutic agents. The main objective of this study was to investigate the effects of nanoliposomal (NL) formulation on enhancing the bioavailability of essential oil. The essential oil of Satureja hortensis (SHO) was encapsulated in nanoliposomes (SHNLs). Physicochemical characterizations of NL formulations (size, charge, polydispersity index [PDI]) were evaluated by dynamic light scattering technique. The nanoliposome encapsulation efficiency (EE) was calculated as 89.90%. The prepared bionanosystems demonstrated significant antibacterial activities against Escherichia coli ATCC 10536, Pseudomonas aeruginosa ATCC 15442, and Staphylococcus aureus ATCC as determined by the agar diffusion method and microdilution tests. Minimum inhibitory concentration (MIC) values for SHNLs were found to be 5.187 µg/µL for E. coli and 2.59 µg/µL for both P. aeruginosa and S. aureus. Importantly, despite the lower substance content, both SHNLs and SHO exhibited comparable antibacterial activity against all tested strains. Furthermore, in order to determine the toxicity profile and possible effects on DNA damage or repair both the genotoxic and antigenotoxic effects of SHNLs were assessed using the cytokinesis-blocked micronucleus (CBMN) method in human lymphocyte cultures. The experimental data collectively indicate that the NL formulation of the S. hortensis essential oil enhances antibacterial activities and provides genoprotective effects against DNA damage. This highlights the significance of liposomal formulations of antioxidants in augmenting their biological activity. The results indicate that SHNLs can be a safe antibacterial agent for the pharmaceutical industry.

Kinetic assessment of iontophoretic delivery efficiency of niosomal tetracycline hydrochloride incorporated in electroconductive gel.

The purpose of this study was to conduct the kinetic assessment of iontophoretic delivery of niosomal tetracycline-HCl formulated in an electroconductive gel. Tween-80 and Span-80 were used to obtain tetracycline-HCl niosomes with an average diameter of 101.9 ± 3.3 nm, a polydispersity index of 0.247 ± 0.004, a zeta potential of - 34.1 mV, and an entrapment efficiency of 70.08 ± 0.16%. Four different gel preparations, two of which contained niosomal tetracycline-HCl, were transdermally delivered using Franz diffusion cells under the trigger effect of iontophoresis, applied at 0.2, 0.5, and 1 mA/cm2 current density. The control group was the passive diffusion results of the preparation made using a tetracycline-HCl-based drug marketed in Turkey. The control group was compared with the groups that contained (a) tetracycline-HCl in an electroconductive gel, (b) the niosomal tetracycline-HCl formulation in water, and (c) the niosomal tetracycline-HCl formulation in the electroconductive gel. The group with the niosomal formulation in the electroconductive gel displayed the highest increase in iontophoretic transdermal delivery relative to the control group, displaying a 2-, 2.1-, and 2.2-fold increase, respectively, by current density. The experimental results of transdermal delivery using the synergistic effect of niosomal formulation in electroconductive gel and the trigger effect of iontophoresis appeared to divert slightly from zero-order kinetics, demonstrating a statistically significant increase in the rate of controlled transdermal drug delivery. Considering that about 20% of the formulation is transdermally delivered in the first half-hour, the iontophoretic transdermal delivery of niosomal tetracycline-HCl can be efficiently used in local iontophoretic therapy.

Antibacterial effects of saliva substitutes containing lysozyme or lactoferrin against Streptococcus mutans.

OBJECTIVE: To determine the antibacterial effects of different saliva-substitutes-containing-lysozyme(LYZ) or-lactoferrin(LF) on Streptococcus mutans(S. mutans) in comparison with human saliva. DESIGN: In vitro wound-healing assay was performed with L929 mouse fibroblast cell line by using various concentrations of LYZ and LF to determine optimum concentrations and to confirm do not show any cytotoxicity of proteins according to cell culture studies. Antibacterial effect was assessed by determining Minimum Inhibitory Concentrations for all groups on S.mutans. Bacterial adhesion of S. mutans for 4 h on hydroxyapatite(HAP) discs after application of different saliva substitutes was evaluated. The formulations were:saliva-substitute(Group SS);saliva-substitute-containing-Lactoferrin(Group SSLF);saliva-substitute-containing-Lysozyme(Group SSLYZ). Human saliva was control group(Group HS). RESULTS: In vitro wound healing assay results showed that, when added into the cell culture media, LYZ and LF significantly increase 48 -h scratch wound closure compared to the cell culture media(p < 0.0001). At the end of second day, samples treated with both between 2.5-100 µg/mL LF and 5-200 µg/mL LYZ were found to have significant wound healing effect(p < 001). It was observed that saliva-substitutes-containing-LYZ or-LF had antibacterial effects on S.mutans. Bacterial adhesion on HAP discs was observed significantly higher in control group than in study groups. The amount of adhered S. mutans was significantly higher in Group SS than other study groups(p < 0.0001). However, no statistically significant difference was found between the number of bacteria adhered to HAP discs between SSLYZ and SSLF groups(p > 0.05). CONCLUSIONS: The study of cell viability and wound healing was great significance in the optimum concentrations of LYZ and LF. Among formulations, saliva-substitutes-containing-LYZ or-LF exhibited higher inhibitory effect on S.mutans.

Next-Generation Natural Baby Barrier Cream Formulations: Physicochemical Analysis and Safety Assessment.

The background of this article is to develop formulations consisting of natural raw materials that are effective in diaper rash by taking advantage of the medicinal properties of zinc oxide, natural oils, and beeswax. The purpose of this research was to determine the appropriate amounts of the constituents of the formulation and to determine the optimum formulation by comparing the margin of safety (MoS), and microbiological and physicochemical properties of the best formulation. For this purpose, parameters such as pH, rheological behavior, hydrophilic and lipophilic balance (HLB), zeta potential, and polydispersity index were analyzed and evaluated to determine the optimum formulation. Besides, microbiological reproduction and 3-month stability studies of the developed product were carried out, and it has been proven that the developed product maintains both microbiological and stability properties throughout its shelf life. Furt hermore, whether each raw material used in the selected optimum formulation remained within MoS values was evaluated according to exposure doses in the literature. Whether it maintains the desired properties throughout the shelf life was evaluated by stability studies. In this article, eight different zinc oxide-based formulations for preventing diaper rash were developed, and their physicochemical properties were examined to optimize cream formulations. baby barrier cream (BBC)-8 was chosen as the ideal formula by comparing all the parameters obtained as a result of the analysis. As a result of the optimization studies of the BBC-8 formulation, the pH value was 7.2, the viscosity property was pseudoplastic-type flow, the particle size was 533.2 nm ± 6.93, and the zeta potential was -30.9 mV ± 0.72. The theoretical safety assessment of each constituent has been made according to the European Union Cosmetics Directives. According to the calculations made on each raw material in BBC-8 according to the directives, the MoS value was found to be more than 230. For the stability studies, no microbiological growth was observed at the end of the 3-month stability studies at 25 and 40°C. In terms of the development of future natural cosmetic product formulations and the defi nition of "natural formulation," it gives hope to prepare a safer cosmetic product for baby rash creams that do not contain preservatives, perfumes, and dyes and consists of natural oils and zinc oxide.

Liposomal Incorporation to Improve Dissolution and Stability of Rosmarinic Acid and Carvacrol Extracted from Oregano (O. onites L.).

The potential antimicrobial benefit of high levels of rosmarinic acid (RA) and carvacrol (CA) in oregano (O. onites L.) extract has been limited until now by poor bioavailability arising from the low aqueous-phase solubility and slow dissolution behaviour of the lyophilized extract (E). To address this issue, various ratios of phospholipon 90H (P90H) and 1,2-dimyristoyl-sn-glycero-3-phospho-(1'-rac-glycerol), sodium salt (DMPG) were sonicated, yielding four empty liposomes (L1, L2, L3, and L90). After an initial selection process, Turkish oregano extract was internalized into the more promising candidates. Each empty liposome, extract-loaded liposome (LE1, LE2, and LE3), and freeze-dried control (E) was assessed in terms of structure, composition, RA and CA dissolution profile, storage stability, and, when relevant, zeta potential. Empty liposome L1, which was prepared using P90H and DMPG in a 1:1 ratio, displayed the most convenient encapsulation traits among the four unloaded types. Loaded liposome LE1, obtained by combining oregano extract and L1 in a 1:1 ratio, proved superior as a vehicle to deliver RA & CA when compared against control freeze-dried E and test liposomes LE2 and LE3. Dissolution profiles of the active compounds RA and CA in loaded liposomes were determined using a semi-automated dissolution tester. The basket method was applied using artificial gastric juice without pepsin (AGJ, 50rpm, 500mL). The pH value was maintained at 1.5 (37 ± 0.5°C). Aliquots (5ml) were manually extracted from parallel dissolution vessels at 1, 3, 5, 7, 10, 15, 20, 25, 30, 45, and 60-minute time points. Dissolution tests, run to completion on LE1, showed that approximately 99% of loaded CA and 88% of RA had been released. Shorter dissolution times were also noted in using LE1. In particular, the release profile of CA and RA had levelled off after only 25 minutes, respectively, depicting an impressive 3.0-3.3 and 2.3-2.6 rate increase compared to the freeze-dried control extract. The improved dispersibility of RA and CA in the form of LE1 was supported by particle size and zeta potential measurements of the liposome, yielding 234.3nm and -30.9mV, respectively. The polydispersity index value was 0.35, indicating a reasonable particle size distribution. To study storage stability, liposomes were stored (4°C, 6 months) in amber coloured glass containers (4 oz.). Each container held 30 capsules, which were stored according to the ICH guidelines prescribed for long-term storage (25°C ± 2°C; 60% ± 5% RH). Triplicate samples were withdrawn after 0, 3, 6, 9, and 12 months for analysis. Lastly, LE1 displayed good storage stability. The results imply that RA and CA can be conveniently and routinely delivered via oral and mucosal routes by first internalizing oregano extracts into appropriately engineered liposomes.

Preformulation, Characterization, and In Vitro Release Studies of Caffeine-Loaded Solid Lipid Nanoparticles.

Encapsulation of active agents in solid lipid nanoparticles (SLNs) is an alternative to other controlled release systems for topical delivery. In this study, caffeine was encapsulated in SLNs to produce a delivery system with controlled release. Caffeine-loaded SLNs (Caf-SLNs) were prepared using the double emulsion method with homogenization and ultrasonication. The characterization studies were performed using dynamic light scattering (DLS), zeta potential, scanning electron microscopy (SEM), and differential scanning calorimetry (DSC) analyses. The encapsulation efficiency tests were performed using UV spectrophotometry. In vitro release studies were conducted using a dialysis bag technique and high-performance liquid chromatography (HPLC) for the quantification of caffeine (Caf). The results from the DLS analysis showed that all formulations had a polydispersity index <0.3 with particle sizes <210 nm. The DSC and SEM results showed that Caf was dispersed in the SLNs. The encapsulation efficiency was 49.22%. The release studies indicated that after an initial burst at 3 min, the SLNs released Caf in a controlled manner over a 6-h period. Taken together, the SLNs can be used as a carrier for the topical delivery of Caf.

Liposome, gel and lipogelosome formulations containing sodium hyaluronate.

The moisture-imparting effect of sodium hyaluronate (Na-HA) was investigated in liposome, gel and lipogelosome topical formulations. Sixteen liposome formulations were prepared with or without Na-HA (45 kDa) using various ratios of dimyristoylphosphatidylcholine, 1,2-dimyristoyl-sn-glycero-3-phosphatidylglycerol, dipalmitoylphosphatidylcholine and phospholipon 100H. The liposomes were characterized in terms of their structure, composition, zeta potential, Na-HA-entrapment capacity and stability. In particular, scanning electron microscopy, polarized light microscopy, dynamic light scattering and atomic force microscopy were utilized to probe appearance, size and size distribution and lamellarity. The work was then extended to gels using the gelling agents poloxamer (PXM 188 or 407) and Carbopol or Ultrez 21 (U-21), yielding liposome-loaded gel formulations (i.e. lipogelosomes). The in vitro release kinetics of Na-HA from liposomes, lipogelosomes and commercial Na-HA reference formulations were studied via a flow-through cell method. Among the liposomal formulations tested, L6, comprising of Na-HA-loaded phospholipon 100H:stearylamine:cholesterol (7:1:2), displayed optimal traits. The mean particle size, zeta potential and entrapment capacity of L6 were determined as 1900 nm, -20.9 mV and 15.0%. The optimum lipogelosome, LG4, was obtained by incorporating liposome L6 into a U-21 gel at a ratio of 1:1 (w/w). In clinical trials, in-house formulations were applied twice daily to 15 female volunteers. The two-week benefits were assessed against a commercial product; and in all cases, changes of skin humidity, sebum content, pH and wrinkle depth were promising. In particular, the LG4 lipogelosome-based formulation had significantly improved skin hydration and compliance, as evidenced by a moisture content gain of 30.4%.