Abstract
Objective: In the present investigation efforts were considered to optimize the different conditions for the preparation of spray dried lactose based proniosomes. The aim of this research was to investigate the feasibility of proniosomes as stable precursors for the development of niosomes as oral drug delivery system for poorly water-soluble drugs.Methods: A total of twenty-eight plain proniosomal formulae were prepared with various surfactant-cholesterol loading ratios in each formula using spray dried lactose as a carrier. Span 20, 40, 60 and 80 were used in various molar ratios with cholesterol. Different evaluation techniques were performed to study the performance of the prepared proniosomes. The micromeritic properties of the prepared proniosomes were analyzed. The reconstituted niosomes were further evaluated for morphological characterization using transmission electron microscope (TEM), particle size analysis, zeta potential, and polydispersity index (PDI). Finally, selected proniosomal formulae were tested for stability study.Results: The proniosomal formulae prepared using span 40 and span 60 exhibited excellent flowability while those prepared with span 20 and span 80 showed poor flow properties. TEM photographs revealed that the vesicles were discrete, spherical without aggregation. The mean vesicle size of reconstituted niosomes was found to be in the range between (252.9±0.43–624.3±0.23 nm) with perfect PDI values (0.387±0.05–0.835±0.03). The negative values of zeta potential indicated that all prepared formulae were stabilized by electrostatic repulsion forces. Stability studies confirmed that proniosomes give a more stable system that could overcome the problems of standard niosomes. Formulae with the smallest particle size, higher surface charge values and best flow properties were selected to be loaded with poorly soluble drugs for further study.Conclusion: The obtained results offered evidence that spray-dried lactose based proniosomes are promising stable drug delivery carriers and ready to incorporate various poorly water-soluble drugs in order to improve their limited oral bioavailability.
Highlights
Over the decades, the oral route remains the most preferred route of administration for drug delivery
The flask was attached to a rotary evaporator (Heidolph, Germany) and the solvent mixture was evaporated under pressure of 600 mmHg at a temperature of 45±2 °C and 60 rpm until spray dried lactose appeared to be dry as a thin powder film on the flask wall [20]
Micromeritic properties of proniosomal formulae were considered as an important parameter as it will affect the uniformity of dose and facility of filling into capsules
Summary
The oral route remains the most preferred route of administration for drug delivery. A plurality of the new and present drugs taken by oral route usually face bioavailability drawbacks [1]. Considerable interest has been focused on the design and formulation of new drug delivery systems. Vesicular drug delivery systems are of high significance. There are different types of vesicular drug delivery systems such as liposomes, niosomes, transferosomes, ethosomes, colloidosomes, and cubosomes. Novel approaches like provesicular drug delivery systems such as proniosomes, layerosomes and ufosomes have been developed which have higher stabilities compared to conventional and simple vesicular systems [3]. Provesicular systems can be used for prolonged and targeted drug delivery with mild side effects and provides patient compliance by decreasing the administered dose
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