Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application-Development, Initial Assessment, and Pilot Release Studies.

Vaginal candidiasis (VC) is an emerging global hardly treated health issue affecting millions of women worldwide. In this study, the nanoemulsion consisting of clotrimazole (CLT), rapeseed oil, Pluronic F-68, Span 80, PEG 200, and lactic acid was prepared using high-speed and high-pressure homogenization. Yielded formulations were characterized by an average droplet size of 52-56 nm, homogenous size distribution by volume, and a polydispersity index (PDI) < 0.2. The osmolality of nanoemulsions (NEs) fulfilled the recommendations of the WHO advisory note. NEs were stable throughout 28 weeks of storage. The stationary and dynamic (USP apparatus IV) pilot study of the changes of free CLT over time for NEs, as well as market cream and CLT suspension as references, were conducted. Test results of the changes in the amount of free CLT released from the encapsulated form were not coherent; in the stationary method, NEs yielded up to 27% of the released CLT dose within 5 h, while in the USP apparatus IV method, NEs released up to 10% of the CLT dose. NEs are promising carriers for vaginal drug delivery in the treatment of VC; however, further development of the final dosage form and harmonized release or dissolution testing protocols are needed.

Effect of a Single and Triple Dose of Levamisole on Hematological Parameters in Controlled Inflammation Model.

This study aimed to evaluate the impact of single and triple administration of levamisole on the dynamics of hematological parameters during experimental pleuritis. The experiment was performed on female Buffalo rats. Rats were randomly assigned to two equal groups that received 1 and 3 doses of levamisole every 2, 24 and 48 h, respectively. Following the experiment, blood samples for the measurement of hematological parameters were collected. The study group receiving three doses of levamisole observed a significant reduction of red blood cell count at 48 h post administration and an increase in mean corpuscular volume compared to the control inflammation group. The administration of a single dose of levamisole results in a significant increase in hematocrit at 72 h, an increase in white blood cell count at 24 h and 72 h, and an increase in neutrophil count at 72 h compared to the control inflammation group. Administration of a single and triple dose of levamisole showed statistically significant modification of some hematological parameters and thus modulates the inflammatory process. In the lungs, this results in a reduction in leukocyte infiltrations around the bronchi and blood vessels.

Emulsion-Based Multicompartment Vaginal Drug Carriers: From Nanoemulsions to Nanoemulgels.

In order to overcome the limitations associated with vaginal administration of drugs, e.g., the short contact time of the drug form with the mucosa or continuous carrier wash-out, the development of new carriers for gynecological use is necessary. Furthermore, high individual anatomical and physiological variability resulting in unsatisfactory therapeutic efficacy of lipophilic active substances requires application of multicompartment drug delivery systems. This manuscript provides an up-to-date comprehensive review of the literature on emulsion-based vaginal dosage forms (EVDF) including macroemulsions, microemulsions, nanoemulsions, multiple emulsions and self-emulsifying drug delivery systems. The first part of the paper discusses (i) the influence of anatomical-physiological conditions on therapeutic efficacy of drug forms after local and systemic administration, (ii) characterization of EVDF components and the manufacturing techniques of these dosage forms and (iii) methods used to evaluate the physicochemical and pharmaceutical properties of emulsion-based vaginal dosage forms. The second part of the paper presents (iv) the results of biological and in vivo studies as well as (v) clinical evaluation of EVDF safety and therapeutic efficacy across different indications.

Dynamic Analysis of Changes of Protein Levels and Selected Biochemical Indices in Rat Serum in the Course of Experimental Pleurisy.

A significant role is played in inflammation by the liver, which, stimulated by inflammatory mediators, synthetizes plasma proteins with various dynamics. The purpose of these studies is to generate a detailed dynamic analysis of changes to concentrations of plasma and serum protein fractions and selected acute-phase proteins as well as nonspecific biochemical indices during the course of an induced pleurisy. The studies were conducted on female inbred Buffalo rats, which were divided into two groups: a control group (C) and an experimental group (IP) in which pleurisy was induced. In the IP group, significant changes in biochemical indices were observed between the 48th and 96th hours of pleurisy. A reduction of albumin, transferrin, urea, and creatinine concentrations was observed, while concentrations of the complement components C3 and C4, haptoglobin, and fibrinogen increased. An early increase of IL-1 was observed, while increases of IL-6 and TNF were noted in the later period. The maximum intensity of the processes described above occurred between the 72nd and 96th hours of pleurisy.

[The composition, biochemical properties and toxicity of snake venoms]. / Sklad i wlasciwosci biochemiczne oraz toksycznosc jadów wezy.

2.5 million cases of snake bites are noticed in the world every year (within 100,000 is mortal). These bites occur frequently in Asia and Africa. Some reports proved the toxicity and composition changes of well-known venoms from the same snake species according to the climatic zone. Snake venom is a natural source of many biologically active substances, including those with potential therapeutic properties. These substances contain peptides, proteins, and enzymes which are divided into five subfamilies: three-finger toxins, serine protease inhibitors of the Kunitz type, phospholipases A2, serine proteases, and metalloproteases. All snake venoms are grouped depending on their mode of action. They usually cause neurotransmission disorders, cardiotoxic action, hemostasis disorders, and have central nervous system and necrotic activity.

Studies on gynecological hydrophilic lactic acid preparations. Part 8: use of chitosan as lactic acid carrier in intravaginal tablets.

Hydrophilic intravaginal tablets based on methylcellulose and containing lactic acid component with chitosan undergo swelling under standard conditions. A high flow-limit of the gel that originates from the tablets as well as its dynamic viscosity should allow for the durable dosage form in the vagina. By choosing the 1:1 ratio of lactic acid to chitosan, it is possible to obtain tablets disintegrating into a gelform at physiological pH range of 3.8-4.4. An increase in the amount of lactic acid in the complex in relation to the polymer up to 2:1 and 3:1 ratios results in gels with a lower pH. These gels possess an acid reserve that might act to neutralize the excess of alkali present in severe vaginal infections.

[Acute, hemorrhagic, overgrowing vaginal inflammation caused by Streptococcus agalacitae--case study]. / Ostre krwotoczne zarastajace zapalenie pochwy wywolane Streptococcus agalactiae - opis przypadku.

The aim of this study was to discuss a case of an acute, hemorrhagic, overgrowing vaginal inflammation caused by Streptococcus agalacitae. Intravaginal globules based on methylcellulose and gelatin, containing a lactic acid and chitosan complex in mole relation 1:1 to 4:1 and, in succesion, an addition of hydrophilisating substances like: PEG-200, propylene-1,2 glycol or glycerol, were applied in the treatment process. The technology was invented in Fac. of pharmacy. Dep. of Pharmaceutical Technology, Wroclaw Medical Univ, Poland (recipe patent-protected).