BackgroundCurcuma longa Linnaeus and Zingiber officinale Roscoe are two main representatives of Zingiberaceae family studied for a wide range of therapeutic properties, including: antioxidant, anti-inflammatory, anti-angiogenic, antibacterial, analgesic, immunomodulatory, proapoptotic, anti-human immunodeficiency virus properties and anticancer effects. This study was aimed to analyse the ethanolic extracts of Curcuma rhizome (Curcuma longa Linnaeus) and Zingiber rhizome (Zingiber officinale Roscoe) in terms of polyphenols, antioxidant activity and anti-melanoma potential employing the B164A5 murine melanoma cell line.ResultsIn order to evaluate the total content of polyphenols we used Folin-Ciocâlteu method. The antioxidant activity of the two ethanolic extracts was determined by DPPH assay, and for the control of antiproliferative effect it was used MTT proliferation assay, DAPI staining and Annexin-FITC-7AAD double staining test. Results showed increased polyphenols amount and antioxidant activity for Curcuma rhizome ethanolic extract. Moreover, 100 μg/ml of ethanolic plant extract from both vegetal products presented in a different manner an antiproliferative, respectively a proapoptotic effect on the selected cell line.ConclusionsThe study concludes that Curcuma rhizome may be a promising natural source for active compounds against malignant melanoma.

Abstract. The aim of the present investigation was to develop and evaluate microemulsion-loaded hydrogels (MEHs) for the topical delivery of fluconazole (FZ). The solubility of FZ in oils, surfactants and cosurfactants was evaluated to identify the components of the microemulsion. The pseudo-ternary phase diagrams were constructed using the novel phase diagram by micro-plate dilution method. Carbopol EDT 2020 was used to convert FZ-loaded microemulsions into gel form without affecting their structure. The selected microemulsions were assessed for globule size, zeta potential and polidispersity index. Besides this, the microemulsion-loaded hydrogel (MEH) formulations were evaluated for drug content, pH, rheological properties and in vitro drug release through synthetic membrane and excised pig ear skin in comparison with a conventional hydrogel. The optimised MEH FZ formulations consisting of FZ 2%, Transcutol P 11.5% and 11%, respectively, as oil phase, Lansurf SML 20-propyleneglycol 52% and 50%, respectively, as surfactant-cosurfactant (2:1), Carbopol EDT 2020 1.5% as gelling agent and water 34.5% and 37%, respectively, showed highest flux values and high release rate values, and furthermore, they had low surfactant content. The in vitro FZ permeation through synthetic membrane and excised pig ear skin from the studied MEHs was best described by the zero-order and first-order models. Finally, the optimised MEH FZ formulations showed similar or slightly higher antifungal activity as compared to that of conventional hydrogel and Nizoral® cream, respectively. The results suggest the potential use of developed MEHs as vehicles for topical delivery of FZ, encouraging further in vitro and in vivo evaluation.

The use of water-soluble polymers of natural, semisynthetic, and synthetic origin for dermal and transdermal drug delivery systems is manifold. Among the most used biopolymers in the formulation of skin preparations, the cellulose ether derivatives as representatives of semisynthetic polymers distinguish through their specific physicochemical properties, by which the pharmacist can select the appropriate cellulose derivative for a particular purpose. The hydrogels containing cellulose derivatives as gelling agents are widely used as water-soluble ointment bases, because they usually associate the characteristics of both conventional and innovative hydrogels, including especially safety, biocompatibility, biodegradability, and a relatively easy way of preparation and low price. The present chapter describes the following issues: the physicochemical properties of water-soluble cellulose derivatives in relationship with their type and grade; physical and chemical properties of cellulose-derivatives-based hydrogels and their compatibility with other auxiliary substances commonly used in the formulation of pharmaceutical hydrogels; the development and manufacturing of these hydrogels on both small and large scales; the characterization of cellulose derivatives hydrogels as pharmaceutical dosage forms through different compendial and noncompendial methods; and well-recognized and novel applications of cellulosederivatives-based hydrogels for dermal and transdermal drug delivery.

A comparative study of 36 molecular descriptors derived from the topological distance matrix and van der Waals space is carried out within this paper. They are partitioned into 16 generalized topological distance matrix indices, 11 topological distance indices known in the literature (seven obtained from eigenvalues/eigenvectors of distance matrix), and 9 van der Waals molecular descriptors. The generalized topological distance indices, k δ λ (λ = 1 -3, k = 1 -4), are introduced in this work on the basis of reciprocical distance matrix. Intercorrelation analysis reveals that topological distance indices mostly contain the same type of information, while van der Waals indices can be bound to the shape or the size of molecules. Furthermore, we found that topological distance indices are good for describing molecular size, and they may be viewed as bulk parameters. The most accurate QSPR models for predicting boiling point of alkanes are based on some of the generalized, eigenvalues/eigenvectors topological distance indices and the van der Waals descriptors of molecular size.

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Biocompatible gel microemulsions containing natural origin excipients are promising nanocarrier systems for the safe and effective topical application of hydrophobic drugs, including antifungals. Recently, to improve fluconazole skin permeation, tolerability and therapeutic efficacy, we developed topical biocompatible microemulsions based on cinnamon, oregano or clove essential oil (CIN, ORG or CLV) as the oil phase and sucrose laurate (D1216) or sucrose palmitate (D1616) as surfactants, excipients also possessing intrinsic antifungal activity. To follow up this research, this study aimed to improve the adhesiveness of respective fluconazole microemulsions using chitosan (a biopolymer with intrinsic antifungal activity) as gellator and to evaluate the formulation variables’ effect (composition and concentration of essential oil, sucrose ester structure) on the gel microemulsions’ (MEGELs) properties. All MEGELs were evaluated for drug content, pH, rheological behavior, viscosity, spreadability, in vitro drug release and skin permeation and antifungal activity. The results showed that formulation variables determined distinctive changes in the MEGELs’ properties, which were nevertheless in accordance with official requirements for semisolid preparations. The highest flux and release rate values and large diameters of the fungal growth inhibition zone were produced by formulations MEGEL-FZ-D1616-CIN 10%, MEGEL-FZ-D1216-CIN 10% and MEGEL-FZ-D1616-ORG 10%. In conclusion, these MEGELs were demonstrated to be effective platforms for fluconazole topical delivery.

To initiate our research into the development of biocompatiîle gelled-microemulsions based on essential oils (EOs) and sucrose esters (SEs) for the topical delivery of fluconazole, this formulation study investigated the usefulness of two relatively harmless natural non-ionic surfactants from the group of SEs (sucrose laurate and stearate) to form, in the presence of antifungal EOs, stable, isotropic microemulsions effective on fluconazole solubilization. Fluconazole’s solubility in EO significantly depended on their chemical composition, showing higher values for cinnamon, oregano and clove essential oils, further selected as oil phase components for microemulsion formulations. The phase behavior of several EO–isopropyl miristate/SE–isopropanol/water systems was assessed through pseudo-ternary phase diagrams constructed by microplate dilution technique. The hydrocarbon chain length of the SE and EO type strongly influenced the size of the microemulsion region in the pseudo-ternary phase diagrams. Ten microemulsion formulations containing 2% fluconazole, 6% or 10% oil mixture of EO–isopropyl myristate in 1:1 ratio, 45% SE-isopropanol mixture and water, were selected and evaluated for physicochemical properties (droplet size, polydispersity, viscosity, refractive index, zeta potential and pH). All formulations were physicochemically acceptable, but viscosity enhancement and further in vitro and in vivo tests are required for the development of biocompatible, clinically safe and effective fluconazole topical preparations.

Betulapendula R. presents an increased interest due to its chemical composition, rich in pentacyclictriterpenes, which are recognized for their remarkable biological activityespecially in the pathologies associated with the cutaneous organ. The present research work was purported to assess the biological activity of two type of birch bark extracts, namely total hydro alcoholic extract (BBE1) and betulin purified extract (BBE2) in terms ofviability ontwo healthy cell lines ( human keratinocytes-HaCat and newborn mice epidermis - JB6Cl41-5a) and two melanoma cell lines (human-A375 and murine-B164A5). Both extracts did not exhibited any toxicity on healthy cells at concentrationsd � 25 �g/mL. BBE1 showed greater efficacy than BBE2 on both melanoma cell lines.