Dramatic improvement in dissolution rate of albendazole by a simple, one-step, industrially scalable technique

Abstract

Low solubility and dissolution rate are the primary challenges in the drug development which substantially impact the oral absorption and bioavailability of drugs. Due to the poor water solubility, Albendazole (ABZ) is poorly absorbed from the gastrointestinal tract and shows low oral bioavailability (5%) which is a major disadvantage for the systemic use of ABZ. To improve the solubility and dissolution rate of ABZ, different classes of hydrophilic excipients such as sugars (lactose, sucrose, and glucose), polyols (mannitol and sorbitol), ionic surfactant (sodium lauryl sulfate) and non-ionic surfactant (Cremophor A25) were co-spray dried with ABZ. The crystallinity changes in the processed drug were characterized by differential scanning calorimetry and X-Ray diffraction methods were used to interpret the enhanced solubility and dissolution rate of the drug. Results showed that the solubility and dissolution rate of ABZ were increased 1.8-2.6 folds and 3-25 folds, respectively. Unexpectedly, SLS decreased the solubility index of drug powder even lower than the unprocessed drug which was attributed to drug-SLS ionic interaction as depicted from Fourier transform infrared spectroscopy. It was concluded that by applying the facile, one-step, industrially scalable technique and the use of small amounts of excipient (only 4% of the formulation), a great improvement (21 folds) in dissolution rate of ABZ was achieved. This finding may be used in the pharmaceutical industries for the formulation of therapeutically efficient dosage forms of class II and IV drugs classified in biopharmaceutical classification system.

Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index

“…Finally, the third parameter of potential discriminating power is simply LogP in variant computations protocols. This is in accord with chemical intuition and pharmaceutical drug delivery strategies (Brough et al, 2015;Ghanbarzadeh et al, 2016;Kalepu and Nekkanti, 2015;Maggi et al, 2013;Sareen et al, 2012;Savjani et al, 2012;Serajuddin, 1999;Sruti et al, 2013) that differences in polarities between drug and excipient is a main driving force toward dissolution. Many examples of such cases can be found in the literature, including cocrystals but also other types of solid mixtures such as inclusion complexes with cyclodextrins (Dua et al, 2011;M Badr-Eldin et al, 2013;Thiry et al, 2017aThiry et al, , 2017b and dispersions with soluble polymers (Brough et al, 2015;Choi and Park, 2017;Ibrahim et al, 2010;Maggi et al, 2013;Six et al, 2004;Thiry et al, 2017a).…”

Avermectins, praziquantel and levamisole have in vitro efficacy against Neoechinorhynchus buttnerae (Neoechinorhynchidae) in Colossoma macropomum: A Serrasalmidae from the Amazon

“…Taraschewski et al (1990) reported that levamisole presented efficacy against N. rutili and E. truttae after 1 hr of exposure. No concentration of albendazole, fenbendazole, mebendazole or loperamide showed in vitro efficacy against N. buttnerae of C. macropomum, since they are poorly soluble in water, resulting therefore in variable and incomplete bioavailability (Ghanbarzadeh et al, 2016;Ibrahim & Al-Anazi, 2013;Pacheco et al, 2018;Romero, Navarro, Sanchez, & Valero, 2014;Taraschewski et al, 1990). Similar inefficacy of albendazole, fenbendazole and mebendazole has also been reported in relation to species of acanthocephalans, nematodes, monogeneans and trematodes parasitizing different fish species (Reimschuessel, Gieseker, & Poynton, 2011;Romero et al, 2014;Taraschewski et al, 1990;Zhang et al, 2014).…”

Exploring the therapeutic potential of sodium deoxycholate tailored deformable-emulsomes of etodolac for effective management of arthritis

“…The observed melting behaviour indicates that the drug is in a crystalline state rather than an amorphous state. The other excipients like PL 90G, Cap MCM C10, Cr A25 and SDC exhibited respective endothermic peaks at 62.32 °C, 29.97 °C, 55.84 °C and 74.55 °C corresponding to their reported melting point 40 , 65 – 67 . Likewise, the developed DE formulation displayed an endothermic peak at 99.89 °C and the disappearance of drug peak may be ascribed to the encapsulation of drug in the interiors of the developed system.…”