Studies on polyhedral niosomes

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The effect of processing variables on the physical characteristics of non-ionic surfactant vesicles (niosomes) formed from a hexadecyl diglycerol ether

Niosomes are vesicles formed by self-assembly of non-ionic surfactants. In this investigation, the effects of processing variables, particularly temperature and sonication, on the physical characteristics and phase transitional behaviour of two niosomal systems based on a hexadecyl diglycerol ether (C(16)G(2)) have been studied. Systems containing C(16)G(2), cholesterol and poly-24-oxyethylene cholesteryl ether (Solulan C24) in the molar ratios 91:0:9 and 49:49:2 were prepared by aqueous dispersion of films, followed by examination of 5(6)-carboxyfluorescein entrapment, particle size and morphology. The thermal behaviour was examined using high sensitivity differential scanning calorimetry (HSDSC) and hot stage microscopy, while the effects of sonication were studied in terms of size and morphology, both immediately after preparation and on storing for 1 h at room temperature and 60 degrees C, Polyhedral niosomes were formed from systems containing C(16)G(2) and Solulan C24 alone, while cholesterol-containing systems formed spherical vesicles mixed with tubular structures; the polyhedral systems were found to have a larger particle size and higher CF entrapment efficiency. HSDSC studies showed the polyhedral systems to exhibit an endotherm at 45.4 degrees C and a corresponding exotherm at 39.1 degrees C on cooling which were ascribed to a membrane phase transition; no equivalent transition was observed for the cholesterol containing systems. Hot stage microscopy showed the polyhedral vesicles to convert to spherical structures at similar to 48 degrees C, while on cooling the spherical vesicles split into smaller. structures and reverted to the polyhedral shape at similar to 49 degrees C. Sonication resulted in the polyhedral vesicles forming spherical structures which underwent a particle size increase on storage at room temperature but not at 60 degrees C. The study suggests that the polyhedral vesicles undergo a reversible transition to spherical vesicles on heating or sonication and that this morphological change may be associated with a membrane phase transition. (C) 2000 Elsevier Science B.V. All rights reserved

Formulation and Optimization of Zidovudine Niosomes

Zidovudine (AZT) is commonly used to treat patients with AIDS, but it is limited by toxicity and high dosing needs. Alternative formulations have been proposed to overcome these drawbacks. The objective of this study was to evaluate process-related variables like hydration and sonication time, rotation speed of evaporation flask, and the effects of charge-inducing agent and centrifugation on zidovudine entrapment and release from niosomes. Formulation of zidovudine niosomes was optimized by altering the proportions of Tween, Span and cholesterol. The effect of process–related variables like hydration time, sonication time, charge-inducing agent, centrifugation and rotational speed of evaporation flask on zidovudine entrapment and release from niosomes was evaluated. The effect of changes in osmotic shock and viscosity were also evaluated. Non-sonicated niosomes were in the size range of 2-3.5 μm and sonicated niosomes formulated with Tween 80 and dicetylphosphate (DCP) had a mean diameter of 801 nm. Zidovudine niosomes formulated with Tween 80 entrapped high amounts of drug and the addition of DCP enhanced drug release for a longer time (88.72% over 12 h). The mechanism of release from Tween 80 formulation was the Fickian type and obeyed first-order release kinetics. Niosomes can be formulated by proper adjustment of process parameters to enhance zidovudine entrapment and sustainability of release. These improvements in zidovudine formulation may be useful in developing a more effective AIDS therapy

Effect of Charged and Non-ionic Membrane Additives on Physicochemical Properties and Stability of Niosomes

The aim of this study was to investigate an influence of different types of membrane additives including negative charge (dicetylphosphate, DCP), positive charge (stearylamine, STR) and non-ionic molecule (cholesteryl poly-24-oxyethylene ether, SC24) on the physicochemical properties of drug-free and drug-loaded niosomes. Salicylic acid having different proportions of ionized and unionized species at different pH was selected as a model drug. The niosomes were composed of 1:1 mole ratio of Span 60: cholesterol as vesicle forming agents. The results show that incorporation of salicylic acid to the niosomes did not affect zeta potential values; however, addition of the membrane additives changed the zeta potential depending on the type of the additives. Transmission electron microscopy revealed that niosomes had unilamellar structure. The particle sizes of all developed niosomes were between 217 to 360 nm. The entrapment efficiency (%E.E.) of all salicylic acid niosomes at pH 3 was higher than that of niosomes at pH 5, indicating that salicylic acid in unionized form was preferably incorporated in niosomes. Furthermore, the positively charged niosomes showed the highest %E.E. of salicylic acid owing to electrostatic attraction between STR and salicylic acid. After 3 months of storage at 4°C, the particle size of the niosomes remained in the nanosize range except for DCP salicylic acid niosomes at pH 3 whose size increased due to an instability of DCP at low pH. In addition, all niosomes showed no leakage of the salicylic acid after 3 months of storage indicating the good stability