Development of poloxamer gel formulations via hot-melt extrusion technology

Mendonsa, Nicole; Murthy, S. N. B.; Hashemnejad, Seyed Meysam; Kundu, Santanu; Zhang, Feng; Repka, Michael A.

doi:10.1016/j.ijpharm.2017.12.008

Cited by 31 publications

(11 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Poloxamer gel has been reported to be of interest in liquid suppository systems, intramuscular drug delivery systems, inner ear drug delivery systems, ocular drug delivery systems, etc. This gel has the potential to be in the liquid state at refrigerated temperatures of 4–5 °C and convert into a gel at body temperature, thereby retarding the release of the drug from the gel (Mendonsa et al, 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Development of thermosensitive poloxamer 407-based microbubble gel with ultrasound mediation for inner ear drug delivery

Liao

Shih

et al. 2021

Drug Delivery

View full text Add to dashboard Cite

Our previous study first investigated feasibility of applying ultrasound (US) and microbubbles (MBs) via external auditory canal to facilitate drug delivery into inner ear. However, most drugs are in aqueous formulae and eliminated via Eustachian tubes after drug application. In this study, feasibility of sustained release of thermosensitive poloxamer 407 (P407)-based MB gel for US mediation-enhanced inner ear drug (dexamethasone, DEX) delivery was investigated. The sol-to-gel transition temperature showed that mixture of DEX and only 10% and 12.5% P407 in MBs can be used for in vitro and in vivo drug delivery experiments. In in vitro Franz diffusion experiments, the release rates of 12.5% P407-MBs þ US groups in the model using DEX as the delivered reagent at 3 h resulted in values 1.52 times greater than those of 12.5% P407-MBs groups. In guinea pigs, by filling tympanic bulla with DEX in 12.5% P407-MBs (DEX-P407-MBs), USMB applied at post-treatment days 1 and 7 induced 109.13% and 66.67% increases in DEX delivery efficiencies, respectively, compared to the group without US. On the 28th day after US-mediated P407-MB treatment, the safety assessment showed no significant changes in the hearing thresholds and no damage to the integrity of cochlea or middle ear. These are the first results to demonstrate feasibility of US-modified liquid form DEX-P407-MB cavitation for enhancing permeability of round window membrane. Then, a gel form of DEX-P407-MBs was generated and thus prolonged the release of DEX in middle ear to maintain the therapeutic DEX level in inner ear for at least 7 days.

show abstract

Section: Introductionmentioning

confidence: 99%

Development of thermosensitive poloxamer 407-based microbubble gel with ultrasound mediation for inner ear drug delivery

Liao

Shih

et al. 2021

Drug Delivery

View full text Add to dashboard Cite

show abstract

“…Further, results of pH, rheology, surface tension, and texture profile analyses showed homogeneity with consistent viscoelastic properties, suggesting excellent gel preparation using HME. Similarly, Mendonsa et al [74] developed polaxomer gel formulations using ketoprofen as a model drug by HME and conventional method. The obtained 30% polaxomer gels were reported to be more ideal than 40% polaxomer gels.…”

Section: Hme For Semisolid Formulationsmentioning

confidence: 99%

An update on the contribution of hot-melt extrusion technology to novel drug delivery in the twenty-first century: part II

Sarabu

Bandari

Kallakunta

et al. 2019

Expert Opinion on Drug Delivery

View full text Add to dashboard Cite

Introduction: Interest in hot melt extrusion (HME) technology for novel applications is growing day by day, which is evident from several hundred publications within the last five years. HME is a cost-effective, solvent free, "green" technology utilized for various formulations with low investment costs compared to conventional technologies. HME has also earned the attention of the pharmaceutical industry by the transformation of this technology for application in continuous manufacturing.Areas covered: Part II of the review focuses on various novel opportunities or innovations of HME such as multiple component systems (co-crystals, co-amorphous systems and salts), twinscrew granulation, semi-solids, co-extrusion, abuse deterrent formulations, solid self-emulsifying drug delivery systems, chronotherapeutic drug delivery systems and miscellaneous applications.Expert opinion: HME is being investigated as an alternative technology for preparation of multi-component systems such as co-crystals and co-amorphous techniques. Twin-screw granulation has gained increased interest in preparation of granules via twin-screw melt granulation or twin-screw dry granulation. This novel application of the HME process provides a promising alternate approach in the formulation of granules and solid dosage forms. However, this technology may need to be further investigated for scalability aspects of these novel applications for industrial production.

show abstract

“…Mendonsa applied HME to mix poloxamer and ketoprofen and then developed a poloxamer gel. The temperatures of the barrel from zones 2–4 were set at 97 °C to ensure the melting of the drug and polymer, with zone 5 at 90 °C, zones 6 and 7 at 80 °C and zone 8 and the die set at 70 °C to ensure the correct form [ 21 ]. Chuah used HPMC, lecithin and isomalt as carriers to prepare an amorphous Cur SD through HME [ 22 ].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Curcumin-Eudragit® E PO Solid Dispersions with Gradient Temperature through Hot-Melt Extrusion

Zhang

Zhu

et al. 2021

Molecules

View full text Add to dashboard Cite

Hot-melt extrusion (HME) has great advantages for the preparation of solid dispersion (SD), for instance, it does not require any organic solvents. Nevertheless, its application to high-melting-point and thermosensitive drugs has been rarely reported. In this study, thermally unstable curcumin (Cur) was used as a drug model. The HME process was systematically studied by adjusting the gradient temperature mode and residence time, with the content, crystallinity and dissolution of Cur as the investigated factors. The effects of barrel temperature, screw speed and cooling rate on HME were also examined. Solubility parameters and the Flory–Huggins method were used to evaluate the miscibility between Cur and carriers. Differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy, equilibrium solubility and in vitro and in vivo experiments were used to characterize and evaluate the results. An amorphous Cur SD was successfully obtained, increasing the solubility and release of Cur. In the optimal process, the mass ratio of Cur to Eudragit® E PO (EPO) was 1:4 and the barrel temperature was set at a gradient heating mode (130 °C–135 °C–140 °C–145 °C–150 °C–155 °C–160 °C) at 100 rpm. Related pharmacokinetic test results also showed the improved bioavailability of the drug in rats. In a pharmacodynamic analysis of Sprague–Dawley rats, the Cmax and the bioavailability of the Cur-EPO SD were 2.6 and 1.5 times higher than those of Cur, respectively. The preparation of the amorphous SD not only provided more solubility but also improved the bioavailability of Cur, which provides an effective way to improve the bioavailability of BCS II drugs.

show abstract

Development of poloxamer gel formulations via hot-melt extrusion technology

Cited by 31 publications

References 29 publications

Development of thermosensitive poloxamer 407-based microbubble gel with ultrasound mediation for inner ear drug delivery

Development of thermosensitive poloxamer 407-based microbubble gel with ultrasound mediation for inner ear drug delivery

An update on the contribution of hot-melt extrusion technology to novel drug delivery in the twenty-first century: part II

Preparation of Curcumin-Eudragit® E PO Solid Dispersions with Gradient Temperature through Hot-Melt Extrusion

Contact Info

Product

Resources

About