Investigating Antiarthritic Potential of Nanostructured Clove Oil (Syzygium aromaticum) in FCA-Induced Arthritic Rats: Pharmaceutical Action and Delivery Strategies.

The combined application of clove oil in a lipid nanocarrier opens a promising avenue for bone and joints therapy. In this study, we successfully developed a tunable controlled-release lipid platform for the efficient delivery of clove oil (CO) for the treatment of rheumatoid arthritis (RA). The ultra-small nanostructured lipid carriers co-loaded with CO (CONCs) were developed through an aqueous titration method followed by microfluidization. The CONCs appeared to be spherical (particle size of 120 nm), stable (zeta potential of -27 mV), and entrapped efficiently (84.5%). In toluene:acetone:glacial acetic acid (90:9:1 percent v/v/v) solvent systems, high-performance thin layer chromatography (HPTLC) analysis revealed the primary components in CO as eugenol (RF = 0.58). The CONCs greatly increased the therapeutic impact of CO in both in vitro and in vivo biological tests, which was further supported by excellent antiarthritic action. The CONC had an antiarthritic activity that was slightly higher than neat CO and slightly lower than standard, according to our data. The improved formulation inhibited serum lysosomal enzymes and proinflammatory cytokines while also improving hind leg function. This study provides a proof of concept to treat RA with a new strategy utilizing essential oils via nanodelivery.

Novel ethosomal gel of clove oil for the treatment of cutaneous candidiasis.

BACKGROUND: Dual-release mechanism of ethosomal gels (ie, ethosomes and gel) makes them as versatile drug delivery systems for topical applications. Clove oil is obtained from the clove buds exhibited broad antifungal and antibacterial activity. Cutaneous candidiasis is the infection caused by Candida albicans or other Candida species. AIM: The aim of the present study was to prepare ethosomal gel of clove oil and evaluate its effectiveness in the treatment of cutaneous candidiasis. METHODS: Ethosomes of clove oil was formulated by using varying concentrations of soyaphosphotidyl choline and ethanol, and later, it was incorporated into carbapol 974 base gels to form ethosomal gel. The prepared ethosomal gels were also evaluated for spreadability, drug release studies, ex vivo permeation study, and antifungal activity. RESULTS: The optimized formulation did not cause any irritation to the skin since the pH of formulation was in the pH range of skin. The ethosomal gel showed satisfactory antifungal activity against the fungus C. albicans compared to pure clove oil. CONCLUSIONS: The results showed that developed formulation could be promising one in the topical delivery of clove oil for the treatment of cutaneous candidiasis.

Nanoemulsion containing 8-methoxypsoralen for topical treatment of dermatoses: Development, characterization and ex vivo permeation in porcine skin.

Oral therapy with 8-methoxypsoralen (8-MOP) may cause major side effects, whereas the topical treatment might not be much effective due to the low penetration induced by typical formulations. Therefore, the objectives of this work are the development and characterization of a nanoemulsion (NE) containing 8-MOP together with an ex vivo permeation study, monitored by a validated HPLC-Fluo method, to determine the amount of drug retained in viable skin (epidermis (E) and dermis (D)) and in stratum corneum (SC). The optimized conditions for NE formulation were achieved by full factorial designs (25 and 32): 60 s and 60% of ultrasound time and potency, respectively; 10 mL of final volume; 2% v/v of oil phase (clove essential oil); and 10% m/v of Poloxamer 407. The NE showed mean droplet diameter of 24.98 ±â€¯0.49 nm, polydispersity index (PDI) of 0.091 ±â€¯0.23, pH values of 6.54 ±â€¯0.06, refractive index of 1.3525 ±â€¯0.0001 and apparent viscosity of 51.15 ±â€¯3.66 mPa at 20 °C. Droplets with nanospherical diameters were also observed by transmission electron microscopy (TEM). Ex vivo permeation study showed that 8.5% of the applied 8-MOP dose permeated through the biological membranes, with flux (J) of 1.35 µg cm-2 h-1. The drug retention in E + D and in SC was 10.15 ±â€¯1.36 and 1.95 ±â€¯0.71 µg cm-2, respectively. Retention in viable skin induced by the NE was almost two-fold higher than a compounded cream (5.04 ±â€¯0.30 µg cm-2). These results suggested that the developed NE is a promising alternative for 8-MOP topical therapy when compared to commercial formulations.

Preparation and Characterization of Chitosan-Based Core-Shell Microcapsules Containing Clove Oil.

The biodegradable microcapsules based on chitosan for a controlled delivery of clove oil were prepared by the single coagulation process. The effect of chitosan concentration, core to shell ratio, types of emulsifier, flocculating agent and hardening agent on the microcapsule diameter and the particle size distribution of microcapsule were investigated. The optimized conditions for the preparation of microcapsules with well-defined structure and narrow dispersibility were under that (1) the concentration of chitosan was 1.0 wt%, (2) clove oil to chitosan ratio was 75:25, (3) OP-10 and 10 wt% sodium sulfate were used as emulsifier and flocculating agent respectively, and (4) the concentration hardening agent glyoxal was 1 wt% based on the weight of chitosan. The uniform spherical structures with smooth surfaces with a particle size distribution of 1-15 µm were evidenced by SEM images of microcapsules. Core-shell, hetero-structures were confirmed by optical micrograph. The chemical component of the microcapsules was determined by FTIR. Thermal analysis showed the microcapsules were thermally stable below 150 degrees C. It was found that the pH value and temperature play important roles on the release rate of clove oil from the microcapsules. The release volume of clove oil from microcapsules at pH = 7, and pH = 10 were smaller than that at pH = 2. And the release volume of Clove oil from microcapsules at 60 degrees C was smaller than that at 20 degrees C and 40 degrees C, which showed a sustained and prolonged release.

[Study on self-microemulsifying drug delivery system of LianXiang prescription].

OBJECTIVE: To prepare self-microemulsifying drug delivery system (SMEDDS) of LianXiang prescription. METHODS: After the test of solubility for the initial screening, surfactants and cosurfactants with certain oil phase were screened through the study of ternary phase diagram and in accordance with the size of self-microemulsifying areas; To screen and optimize the self-microemulsifying formulation, the influence of related factors such as the ingredients of the prescription and dilution media on the self-microemulsifying areas were tested, and the particle dimension of microemulsion was determined. The tests of self-microemulsifying rate and stability were carried out to evaluate the formulation. RESULTS: The total alkaloid of Coptis chinensis--the essential oil of Eugenia caryophyllata-Cremophor RH60-1,2-propylene glycol(40: 20: 60: 20, w/w) was the optimal formulation; it had good self-microemulsifying efficiency and stability, and its microemulsion had smaller particle dimension and polydispersity index (17.4 nm, 0.176). CONCLUSION: The optimal formulation can be used as SMEDDS of LianXiang prescription for follow-up researches.