Sugar coated ceramic nanocarriers for the oral delivery of hydrophobic drugs: formulation, optimization and evaluation

Abstract

In order to enhance the delivery of poorly-soluble drugs, we have explored aquasomes (three-layered, ceramic core based, oligosaccharide coated nanoparticles) as potential carriers for the delivery of model hydrophobic drug piroxicam (log P = 3.1). Ceramic nanoparticles were prepared using two techniques; namely, co-precipitation by refluxing and co-precipitation by sonication. Core preparation was finally done using sonication approach; based on the higher % yield (42.4 ± 0.4%) and shorter duration (1 day) compared to the reflux method (27.4 ± 2.05%, 6 days). Lactose loading onto ceramic core was achieved using adsorption. Colorimetric analysis of lactose coating was done using Anthrone method. Optimization of process variables namely, incubation time and core to coat ratio (for sugar loading) was carried out. Optimum time of incubation was 3 h and the core to coat ratio was 4:1. The drug loading was achieved by incubating the sugar loaded cores in different concentrations of piroxicam solution and it was found that 1.5% w/v piroxicam was optimal. Structural characterization using Fourier-Transform Infra Red Spectroscopy (FTIR) confirmed the presence of sugar coating onto the core. Morphological evaluation using transmission electron microscopy (TEM) revealed spherical nanoparticles (size 56.56 ± 5.93 nm for lactose coated core and 184.75 ± 13.78 nm for piroxicam loaded aquasomes) confirming the nanometric dimensions.

Aquasomes: Self-assembled systems for the delivery of bioactive molecules

“…Lactose coating can also be done by adsorption by direct incubation and by nonsolvent addition. [7] Drug loading The surface modified nanocrystalline cores provide the solid phase for the subsequent nondenaturing self-assembly for broad range of biochemically active molecules. The drug can be loaded by partial adsorption.…”

“…By using the principle of self-assembly, the aquasomes are prepared in three steps, i.e., preparation of core, coating of core, and immobilization of drug molecule. [3,7,11] Preparation of the core The first step of aquasome preparation is the fabrication of the ceramic core. The process of ceramic core preparation depends on the selection of the materials for core.…”

“…Other disaccharides that exhibit similar dehydroprotectant activity include cellobiose, and ironically, sucrose; other oligosaccharide-type molecules such a maltose, sorbitol, lactitol also appear to exhibit dehydroprotectant activity. [7,8] Trehalose and related dissacharides such as cellobiose, if immobilized properly on nanoparticulate substrates could prevent the surface-induced desiccation process that tends to affect the activity of biochemical substances. Carbohydrate film on ceramic particle retains the drugs spatial properties, for example, three-dimensional conformations, a freedom of internal molecular rearrangement induced by intermolecular interactions, and a freedom of bulk movement.…”

Lipids and inorganic nanoparticles in oral insulin delivery

“…This property of maintaining the conformational integrity of bioactive molecules shows that aquasomes have potential as a carrier system for delivery of peptides/proteins. Aquasomes have been explored for the delivery of insulin, haemoglobin and various antigens [121,122].…”

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“…The cores were fabricated by a procedure as proposed by Kossovsky et al by the reaction of disodium hydrogen phosphate with calcium chloride to yield the colloidal precipitate [19,37,38] with little modification. Based on the reaction stoichiometry, equivalent moles were reacted in a reaction volume of 120 ml specifically, disodium hydrogen phosphate (1 mole = 8.90 g) and calcium chloride (1 mole = 7.35 g) were taken in 60 ml of water each separately and mixed.…”