Development and evaluation of long-acting epidural “smart” thermoreversible injection loaded with spray-dried polymeric nanospheres using experimental design

Abstract

Context: Reduction of injection frequency as well as localization of drug absorption in the injection site are important requirements in epidural pain treatment. Purpose: Our objective is to explore the production feasibility of controlled release thermoresponsive spray-dried tramadol HCl (TmH) nanospheres for localized epidural injection. Methods: A 2 4 factorial design was employed to study the effect of some selected variables. Results: F15 having the most extended release (MDT = 89.03 ± 0.76 min) was selected, based on regression analysis, for further investigation and characterization. The selected nanospheres (particle diameter = 832.5 ± 10.61 nm) with good flowing properties (θ = 28.076 ± 1.20) was reconstituted with different concentrations of Poloxamer 407 (P407) solution. The optimum reconstituted F15 nanospheres, prepared using 20% w/w P407, was liquid at room temperature, exhibited sol-gel transition at 37°C, was easily withdrawn and injected using 23G needle. The evaluation of the analgesic effect of the selected formula using hot plate method showed a desired rapid onset, yet, extended analgesic effect up to 24 h. The AUC 0-24 h (2998.072 ± 61.830) as well as E max (200.788 ± 12.123) were significantly higher than drug solution and control while T max (2.200 ± 1.095) was non-significant compared to both. Conclusion: the designed formula offers a promising approach as safe depot epidural analgesic.

A Novel Method for Preparing Surface-Modified Fluocinolone Acetonide Loaded PLGA Nanoparticles for Ocular Use: In Vitro and In Vivo Evaluations

“…This finding confirms the presence of entanglement between PLGA nanoparticles and its chitosan HCl coat indicating an efficient and stable coat (46). The endothermic characteristic peak of fluocinolone acetonide was not detected in the nanoparticles thermograms, suggesting the absence of the drug crystalline state and the formation of a molecular dispersion of the drug in the formulated colloids (30,47).…”

“…XThe higher entrapment of drug in the supernatant of the selected chitosan HCl surface-modified PLGA nanoparticles (Cs1-F2; Table VI) is reflected in the obtained high release results. The increase of drug concentration in the nanoparticles can increase the concentration gradient which is an important release driving force and can, therefore, lead to increase the diffusion rate of the drug out of the preparation (47). Also, the diffusion of the drug out from the nanoparticles can be enhanced by the hydrophilic properties of chitosan HCl molecules attracting water to penetrate inside the nanoparticles.…”

Calcium-Enriched Nanofibrillated Cellulose/Poloxamer in-situ Forming Hydrogel Scaffolds as a Controlled Delivery System of Raloxifene HCl for Bone Engineering

“…After injection, P407 gels act as depot at the application site, increase drug residence time, prolong drug release leading to an improved drug bioavailability and efficacy. [27][28][29][30][31] Also, P407 is FDA approved for parenteral use due to its low toxicity. 32 Raloxifene hydrochloride (RLX) is a selective estrogen receptor modulator (SERM) utilized in osteoporosis.…”

Nanotherapeutics as promising approaches to combat fungal infections

“…In addition, most of them have intrinsic bioadhesive properties due to the pres- Kamel, Basha, & El Awdan, 2013;Ludwig, 2005;Valenta, 2005). In addition, most of them have intrinsic bioadhesive properties due to the pres- Kamel, Basha, & El Awdan, 2013;Ludwig, 2005;Valenta, 2005).…”

“…Natural polymers provide some advantages related to low cost, availability, biocompatibility, safety, and low side effects. In addition, most of them have intrinsic bioadhesive properties due to the presence of some functional group in their structure, this enables them to be of great interest in drug delivery through almost all routes of Kamel, Basha, & El Awdan, 2013;Ludwig, 2005;Valenta, 2005).…”