Abstract
The main objective of this study was to compare the powder property, dissolution and bioavailability of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG)-loaded self-emulsifying granule system (SEGS) and solid self-nanoemulsifying drug delivery system (SNEDDS). Various SEGS formulations were prepared, and the effect of surfactant and binder on the drug solubility in them, leading to selecting sodium lauryl sulphate (SLS) and hydroxyl propyl methyl cellulose (HPMC). The SEGS and SNEDDS were prepared with PLAG/SLS/HPMC/calcium silicate/microcrystalline cellulose at the weight ratio of 1:0.25:0.1:0.5:3 employing the fluid bed granulation and spray-drying technique, respectively. Their powder properties were compared in terms of flow ability, emulsion droplet size, scanning electron microscopy, and powder X-ray diffraction. Furthermore, the solubility, dissolution, and oral bioavailability in rats of the SEGS were assessed in comparison with the SNEDDS. The SEGS and SNEDDS enhanced the solubility of the drug approximately 36- and 32-fold as compared with the drug alone; but they had no differences. The crystalline drug may exist in both the calcium silicate and microcrystalline cellulose (MCC) in the SEGS, but only in the calcium silicate in the SNEDDS. The SEGS had considerably improved the flow ability (Hausner ratio, 1.23 vs. 1.07; Carr index, 19.8 vs. 43.5%) and drug dissolution as compared with the SNEDDS. The SEGS and SNEDDS with double peak profiles, unlike the single peak of drug alone, showed a significantly higher plasma concentration and area under the curve (AUC), as compared with drug alone. Although they were not significantly different, the SEGS gave higher AUC than did the SNEDDS, suggesting its enhanced oral bioavailability of PLAG. Thus, the SEGS could be used as a powerful oral dosage form to improve the flow ability and oral bioavailability of PLAG, an oily drug.
Highlights
The oily drug, 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG, Figure 1), was originally isolated from seed oils, bovine udder, and deer horns
Owing to its oily properties, PLAG is practically insoluble in water, resulting in low oral bioavailability [11]
The flow ability and bioavailability of oily drugs such as PLAG can be greatly improved by formulation into self-emulsifying granule system (SEGS) using fluid bed granulation
Summary
The oily drug, 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG, Figure 1), was originally isolated from seed oils, bovine udder, and deer horns. The self-emulsifying drug delivery systems, drug-loaded blends of oils, surfactants, and co-surfactants, can be used to increase dissolution and absorption due to the spontaneous formation of a submicron droplet size. Conventional self-emulsifying drug delivery systems are filled into soft gelatin capsules (liquid form) and are associated with problems related to production costs, stability, storage, and reproducibility [12]. These difficulties can be avoided by preparing solid self-emulsifying drug delivery systems that focus on the incorporation of liquid and semi-solid to solid forms, employing various solidification processes, such as adsorption to solid carriers [13], spray-drying [14], and nanoparticle technology [15]. The fluid bed granulation process is a versatile approach for obtaining solid granule forms [18]
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