Preparation and physicochemical evaluation of transdermal aerosols containing ketoprofen

Purpose: To prepare transdermal ketoprofen metered-dose aerosol formulations containing menthol and isopropyl myristate (IPM) as penetration enhancers and to evaluate their physicochemical and permeation properties.Methods: Selected ratios of ketoprofen, ethanol, polyvinylpyrrolidone K30 (PVP K30, anti-nucleant), and penetration enhancers were mixed and filled into aluminum aerosol cans with hydrofluoroalkane- 134a as propellant. The physicochemical properties of the films, and their ex vivo permeation properties in rat skin were investigated over a 24-h period. Rat skin was exposed to a definite dose of each ketoprofen film to determine the quantity of drug in the receptor compartment over a 24-h period.Results: All the transdermal formulations showed good integrity and film uniformity. Formulations with permeation enhancers presented higher rates of skin penetration compared to control formulations. Formulations containing 3% PVP and 5% IPM produced the highest permeation rates (Jss, 85.35 μg/cm2/h).Conclusion: These results indicate that incorporation of antinucleant polymer and permeation enhancers in aerosols containing ketoprofen enhances aerosol stability and drug permeation through rat skin.Keywords: Ketoprofen, Antinucleant, Permeation enhancer, Topical aerosol, Transdermal deliver

Evaluation of the doxycycline release from AH26 sealer-doxycycline combination: An ex vivo study

INTRODUCTION: The purpose of this ex vivo study was to determine the releasing characteristics and doxycycline dentinal diffusion of AH26 sealer-doxycycline combination from apical 3mm of tooth root and apical foramen.MATERIALS & METHODS: One-hundred and two recently extracted single-rooted human teeth were decoronated and prepared with #3 and #4 Gates-Glidden drills and rotary Mtwo files. Smear layer was removed; all surfaces except for apical 3mm of each root were sealed with two coats of nail polish. To quantify the release and diffusion of the doxycycline at different time intervals (30 min, 48 and 72 h) after root canal obturation, the samples were randomly divided into three groups (n=30; 0.5 h, 48 h, 72 h). To evaluate the release of doxycycline from AH26 sealer-doxycycline combination at six concentrations of antibiotic including 0.5%, 1%, 2%, 5%, 10% and 20%; each experimental group was divided into six equal subgroups (n=5). Root canals were filled with gutta-percha and AH26-doxycycline combinations and then were placed in vials containing 1.25mL of phosphate buffer saline solution (PBS). After 30 min, 48 and 72 h, the amount of doxycycline released from specimens into PBS were determined by measuring the absorbance values using UV spectrophotometry at λmax=350 nm. Data were analyzed using two-way ANOVA. RESULTS: The findings of this study revealed that AH26 sealer-doxycycline combination released variable measures of antibiotic at each time interval and in the various concentrations. At 30 min, no statistically significant differences were obtained between the results of subgroups, but at 48 and 72 h these differences were significant (P < 0.001). The results also showed that differences between 0.5 h, 48 h and 72 h were significant within subgroups (P < 0.01). CONCLUSION: Under the conditions of this ex vivo study, doxycycline can be released from AH26 sealer-antibiotic combination through 3mm of apical root and apical foramen at 30 min, 48 and 72 h after mixing the sealer with doxycycline at concentrations of 0.5% up to 20%.

Nano-niosomes in drug, vaccine and gene delivery: a rapid overview

  Abstract Niosomes, non-ionic surfactant vesicles (NSVs), are the hydrated lipids composed mainly of different classes of non-ionic surfactants, introduced in the seventies as a cosmetic vehicle. Nowadays, niosomes are used as important new drug delivery systems by many research groups and also they are effective immunoadjuvants which some commercial forms are available in the market. These vesicles recently used as gene transfer vectors as well. This review article presents a brief report about the achievements in the field of nanoscience related to NSVs. Different polar head groups from a vast list of various surfactants with one, two or three lipophilic alkyl, perfluoroalkyl and steroidal moieties may be utilized to form the proper vesicular structures for encapsulating both hydrophilic and hydrophobic compounds. The methods of niosome preparation, the vesicle stability related aspects and many examples of pharmaceutical applications of NSVs will be presented. The routes of administration of these amphiphilic assemblies are also discussed.

Preparation and Evaluation of Inhalable Itraconazole Chitosan Based Polymeric Micelles

Background: This study evaluated the potential of chitosan based polymeric micelles as a nanocarrier system for pulmonary delivery of itraconazole (ITRA).Methods: Hydrophobically modified chitosan were synthesized by conjugation of stearic acid to the hydrophilic depolymerized chitosan. FTIR and 1HNMR were used to prove the chemical structure and physical properties of the depolymerized and the stearic acid grafted chitosan. ITRA was entrapped into the micelles and physicochemical properties of the micelles were investigated. Fluorescence spectroscopy, dynamic laser light scattering andtransmission electron microscopy were used to characterize the physicochemical properties of the prepared micelles. The in vitro pulmonary profile of polymeric micelles was studied by an air-jet nebulizer connected to a twin stage impinger.Results: The polymeric micelles prepared in this study could entrap up to 43.2±2.27 μg of ITRA per milliliter. All micelles showed mean diameter between 120–200 nm. The critical micelle concentration of the stearic acid grafted chitosan was found to be 1.58×10-2 mg/ml. The nebulization efficiency was up to 89% and the fine particle fraction (FPF) varied from 38% to 47%. The micelles had enough stability to remain encapsulation of the drug during nebulization process.Conclusions: In vitro data showed that stearic acid grafted chitosan based polymeric micelles has a potential to be used as nanocarriers for delivery of itraconazole through inhalation