Sucrose Stearate-Enriched Lipid Matrix Tablets of Etodolac: Modulation of Drug Release, Diffusional Modeling and Structure Elucidation Studies

Abstract

Etodolac is a non-steroidal anti-inflammatory drug having an elimination half-life of 7 h; oral doses are given every 6-8 h. The aim of current work was the development of controlled-release etodolac lipid matrix tablets. The variables influencing design of these tablets (L1-L28) by the hot fusion method were investigated including; (1) lipid type (stearic acid, cetyl alcohol, cetostearyl alcohol, Imwitor® 900K, Precirol® ATO 5 and Compritol® ATO 888), (2) drug/lipid ratio (1:0.25 and 1:0.50, respectively), (3) filler type (lactose, Avicel® PH101 and their physical mixtures; 2:1, 1:1, and 1:2, respectively), (4) surfactant's HLB (5 and 11), and (5) drug/surfactant ratio (20:1 and 10:1, respectively). Statistical analysis and kinetic modeling of drug release data were evaluated. The inner matrix of the tablet was visualized via scanning electron microscopy (SEM). An inverse correlation was observed between the drug/lipid ratio and the drug release rate. Precirol®- and Compritol®-containing formulae showed more retarded drug release rates. Lactose/Avicel® physical mixture (1:1) was considered as a filler of choice where it minimized the burst effect observed with Avicel®-free formulae. The higher surfactant's HLB, the higher drug release rate. The similarity factor (f(2)) between the drug release profiles revealed similarity within the investigated drug/surfactant ratios. Sucrose stearate D1805®-based matrix (L21) succeeded in delivering more than 90% of etodolac over 12 h, following anomalous (non-Fickian) controlled-release kinetics. SEM micrographs confirmed pore formation, within the latter matrix, upon contact with dissolution medium.

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“…These results correlated with the imperfect matrix structure of Precirol ATO 5 ® and Compritol 888 molecules, which are formed due to the mono-, di-, and triglyceride contents that impart loose, highly porous structural characteristics, which allows easier accommodation and higher solubility of the drug. 39 Precirol ATO 5 ® is palmitostearate glyceride mixture while Compritol 888 is behenate glyceride mixture; 40 the diversity of Precirol ATO 5 ® fatty acid content with subsequent looser structure explain its higher drug entrapment ability than Compritol 888, so it was selected to be used as lipid core for the preparation of NAT-SLNs in this study. 38 For SAA selection, SLN formulations alone were prepared using different SAAs and evaluated for PS, ZP, PDI, and precipitation.…”

Formulation and In Vitro and In Vivo Evaluation of Lipid-Based Terbutaline Sulphate Bi-layer Tablets for Once-Daily Administration

“…Wide arrays of wax-lipid based hydrophobic materials are available for sustaining drug action as Compritol® 888 ATO (glyceryl behenate) [19][20][21], Precirol® ATO 5 (glyceryl palmito-stearate) [22][23][24], stearic acid [23][24][25], and tristearin [26].…”

Comparative Study of Glyceryl Behenate or Polyoxyethylene 40 Stearate-Based Lipid Carriers for Trans-Resveratrol Delivery: Development, Characterization and Evaluation of the In Vitro Tyrosinase Inhibition

“…Behanic acid is a fatty acid with a longer chain length (C22 fatty acid) than either stearic acid (C18 fatty acid). Furthermore, the longer the chain length of the former would ensure a higher degree of lipophilicity [28]. Noteworthy, the polydispersity index (PdI) is a parameter related to particle size distribution and, in this context, PdI values higher than 0.7 indicates very broad distribution, while PdI values close to 0.2 are usually associated with more homogeneous particle size distribution [29].…”