Amorphous solid dispersions of hecogenin acetate using different polymers for enhancement of solubility and improvement of anti-hyperalgesic effect in neuropathic pain model in mice

RETRACTED ARTICLE: Poloxamer-407-Co-Poly (2-Acrylamido-2-Methylpropane Sulfonic Acid) Cross-linked Nanogels for Solubility Enhancement of Olanzapine: Synthesis, Characterization, and Toxicity Evaluation

“…Poor soluble drugs are eliminated from gastrointestinal tract (GIT) prior their dissolution which result in low bioavailability and reduce therapeutic effects. Different strategies have been explored to increase the solubility, dissolution, and ultimately the bioavailability of chemical agents belonging to biopharmaceutical classification system II and IV (BCS II, IV) (4) such as hydrogels, amorphous solid dispersions, co-crystallization, nanocrystals, liposome, solid lipid nanoparticles (SLNs), micronization, supercritical fluid (SCF) process, utilization of surface tension lowering agents, nanosuspension, nanoemulsion, production of liquid-solid formulations, micellar solubilization, self-emulsifying drug delivery systems (SEDDS), hydrotrophy, inclusion complexation with cyclodextrins, modification of pH, and co-solvency techniques (3,(5)(6)(7)(8)(9)(10)(11)(12)(13).…”

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

“…Neuropathic pain is a state of chronic pain caused by lesions or diseases of the somatosensory nervous system [ 77 ], for the treatment of which different drugs are used, which; however, have shown inconsistent results. To develop alternative therapies, among the pharmacological activities attributed to hecogenin acetate, the analgesic one has proven interesting in the treatment of chronic pain [ 78 ].…”

“…To develop alternative therapies, among the pharmacological activities attributed to hecogenin acetate, the analgesic one has proven interesting in the treatment of chronic pain [ 78 ]. In this context Moreira et al [ 77 ] developed solid dispersions with hydrophilic polymers, namely PVP K30, PEG 6000, HPMC, Soluplus ® and PVP/VA 64, to increase the solubility of this drug and improve its dissolution profile. In this study, the anti-hyperalgesic activity of SDs was evaluated in vivo in mice selected as a neuropathic pain model.…”

The search for translational pain outcomes to refine analgesic development: Where did we come from and where are we going?

“…It is worth noting that grip strength is also used to monitor functionality after recoverable sciatic nerve injury (crash injury) (e.g. Martins et al, 2018;de França Almeida Moreira et al, 2018), and although these studies are not usually designed to use this measure as a pain index (and were therefore not included in our analysis), in view of the variety of pain models which are sensitive to decreased in grip strength, researchers aiming to investigate nerve regeneration should be aware of the influence of pain on this outcome since it may negatively influence the apparent functional recovery. Conversely, grip strength cannot be used as a pain outcome in most standard models of neuropathic pain which involve surgical injury to the sciatic nerve, because the motor nerve lesions prevent the animals from gripping.…”