Comparative study between synthetic and phospholipids of natural origin: effect of phospholipid selection on the behavior of a topical liposomal dosage form incorporating terbinafine

Abstract

Selection of excipients used is a critical step in the design of a pharmaceutical dosage form as it affects its behavior upon application, as during storage. The purpose of the present study is to evaluate and compare the behavior of six liposomal formulations intended for topical application composed of two widely used phospholipids 1,2-diacyl-sn-glycero-3-phosphocholine and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine with and without incorporation of cholesterol. Liposomal hydrogels made of hydroxyethylcellulose 3% and incorporating the anti-fungal agent terbinafine hydrochloride (E)-N-(6,6-dimethyl-2-hepten-4-inyl)-N-methyl-1-naphthalene-methanamine (-hydrochloride) were prepared, their viscosity was measured and in vitro drug release was studied. Moreover, physical stability and drug retention during storage at two different temperatures (2-8 °C and RT) were examined over time. The results showed differences in the behavior between the two phospholipids while incorporation of cholesterol at the studied concentrations was found to be of minor importance. Drug release was found to be favorable from 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) liposomal hydrogels and drug retention was found to be higher at lower storage temperature for all batches. Original physicochemical properties of all batches were found to be retained at least for a week.

Release of Tretinoin Solubilized in Microemulsion from Carbopol and Xanthan Gel: In Vitro versus Ex Vivo Permeation Study

“…SpectraPor ® is not a routinely used or validated membrane such as Strat-M or other equivalents for in vitro drug release studies. However, it was used in several in vitro permeation studies, according to which we proceeded [ 54 , 55 ].…”

Synthetic phospholipids with high purity fatty acids

“…This higher purity and analytical uniformity of synthetic phospholipids is crucial for reproducible drug formulation production processes and batch‐to‐batch consistent drug product quality. Additionally, higher purity single products can potentially show better efficiency in the final application due to fewer unspecific interactions with contaminants . Disadvantages of synthetic phospholipids can be their long routes of production; however, this can be offset if multiple commercial phospholipids are incorporated into a single synthesis strategy.…”