Investigation of Formulation Variables and Excipient Interaction on the Production of Niosomes

Abstract

Abstract. The aim of this study was to investigate the effects of formulation and process variables on the properties of niosomes formed from Span 40 as nonionic surfactant. A variety of formulations encapsulating Paclitaxel, a hydrophobic model drug, were prepared using different dicetyl phosphate (DCP) and Span 40-cholesterol (1:1) amounts. Formulations were optimized by multiple regression analysis to evaluate the changes on niosome characteristics such as entrapment efficiency, particle size, polydispersity index, zeta potential and in vitro drug release. Multiple regression analysis revealed that as Span 40-cholesterol amounts in the formulations were increased, zeta potential and percent of drug released at 24th hour were decreased. Besides, DCP was found to be effective on increasing niosome size. As a process variable, the effect of sonication was observed and findings revealed an irreversible size reduction on Span 40 niosomes after probe sonication. Monodisperse small sized (133±6.01 nm) Span 40 niosomes entrapping 98.2% of Paclitaxel with a weight percentage of 3.64% were successfully prepared. The drugexcipient interactions in niosomes were observed by differential scanning calorimetry and X-ray powder diffraction analysis. Both techniques suggest the conversion of PCTs' crystal structure to amorphous form. The thermal analyses demonstrate the high interaction between drug and surfactant that explains high entrapment efficiency. After 3-month storage, niosomes preserved their stability in terms of drug amount and particle size. Overall, this study showed that Span 40 niosomes with desired properties can be prepared by changing the content and production variables.

Calcium alginate microspheres containing metformin hydrochloride niosomes and chitosomes aimed for oral therapy of type 2 diabetes mellitus

“…The selected Span 1 60/CH/DCP niosomal dispersion was then subjected to sonication, for different times and power intensity, in order to find the best conditions to suitably further reduce the vesicle dimensions (Sezgin-Bayindir and Yuksel, 2012). The results, summarized in Table 3, showed that 2 h sonication at 100 W caused an about 3 times reduction of vesicle particle size, without affecting the drug entrapment efficiency.…”

Formulation of Span 80 niosomes modified with SDS for lactic acid entrapment

“…(2014) [1][2][3][4][5][6][7][8][9][10][11][12][13] www.deswater.com doi: 10.1080/19443994.2014.993726 attractiveness of these vesicles for industrial production [10,11]. Encapsulation efficiency depends on several factors such as the type of structure (multilamellar, unilamellar, or multivesicular), the length of the hydrophobic group of surfactant forming the bilayer, the nature and size of the hydrophilic head, pH and composition of the formulation medium, and the nature of the solute (hydrophobicity, polarity, molecular weight, and structure).…”

Lactic acid recovery by microfiltration using niosomes as extraction agents

“…Moreover, their large-scale production without using unacceptable solvents is uncomplicated, so they are widely used in pharmaceutical, cosmetic and, to a lesser extent, food applications [19][20][21][22][23]. Another advantage for industrial production of these vesicles is the large number of non-toxic and relatively low-cost non-ionic surfactants available for niosome formulation [24]. Encapsulation efficiency depends mainly on niosome structure, the nature and size of the hydrophilic head and the length of the hydrophobic group of surfactant forming the bilayer, pH and composition of the formulation medium, and the nature of the solute [25][26][27].…”