Influence of hydroxypropyl methylcellulose, methylcellulose, gelatin, poloxamer 407 and poloxamer 188 on the formation and stability of soybean oil-in-water emulsions

(1) Background: Clozapine is the most effective antipsychotic. It is, however, associated with many adverse drug reactions. Nose-to-brain (N2B) delivery offers a promising approach. This study aims to develop clozapine-encapsulated thermosensitive sol–gels for N2B delivery. (2) Methods: Poloxamer 407 and hydroxypropyl methylcellulose were mixed and hydrated with water. Glycerin and carbopol solutions were added to the mixture and stirred overnight at 2–8 °C. Clozapine 0.1% w/w was stirred with polysorbate 20 (PS20) or polysorbate 80 (PS80) at RT (25 °C) before being added to the polymer solution. The final formulation was made to 10 g with water, stirred overnight at 2–8 °C and then adjusted to pH 5.5. (3) Results: Formulations F3 (3% PS20) and F4 (3% PS80) were selected for further evaluation, as their gelation temperatures were near 28 °C. The hydrodynamic particle diameter of clozapine was 18.7 ± 0.2 nm in F3 and 20.0 ± 0.4 nm in F4. The results show a crystallinity change in clozapine to amorphous. Drug release studies showed a 59.1 ± 3.0% (F3) and 53.1 ± 2.7% (F4) clozapine release after 72 h. Clozapine permeated after 8 h was 20.8 ± 3.0% (F3) and 17.8 ± 3.1% (F4). The drug deposition was higher with F4 (144.8 ± 1.4 µg/g) than F3 (110.7 ± 2.7 µg/g). Both sol–gels showed no phase separation after 3 months. (4) Conclusions: Binary PS80-P407 mixed micelles were more thermodynamically stable and rigid due to the higher synergism of both surfactants. However, binary mixed PS20-P407 micelles showed better drug permeation across the nasal mucosa tissue and may be a preferable carrier system for the intranasal administration of clozapine.

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Valuing Best Poloxamer Carrier for Meloxicam Solid Dispersions by novel microwave fusion: Designing and Characterization

Abasyn Journal Life Sciences ◽

10.34091/ajls.2.1.1 ◽

2019 ◽

pp. 1-15

Keyword(s):

Solid Dispersions ◽

Physicochemical Characterization ◽

Poloxamer 407 ◽

Research Activity ◽

Fusion Technique ◽

Poloxamer 188 ◽

Tablet Compression ◽

Tablet Formulations

Present research activity is to establish the best Poloxamer carriers for making solid dispersions (SD) with Meloxicam. The main aim of this investigation is to find the best among the better Poloxamer carriers viz., Poloxamer-108, Poloxamer-188, Poloxamer-237, Poloxamer-338 and Poloxamer-407 for making SD by novel microwave fusion technique. Four portions of Meloxicam: Poloxamer in various ratios (1:1, 1:2, 1:4 and 1:6) are used for making SD by microwave fusion technique later compressed using 8 station tablet compression machine. The SD and tablet formulations are evaluated for physicochemical characterization. All the prepared batches found to have satisfactory specifications as per pharmacopoeia. The authors concluded that Poloxamer-188 is found to be the best carrier among the Poloxamer carriers used for making Meloxicam SD. Keywords: Meloxicam, Poloxamer, microwave, solid dispersions, tablets

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Poloxamer 407-Based Thermosensitive Emulgel as a Novel Formulation Providing a Controlled Release of Oil-Soluble Pharmaceuticals—Ibuprofen Case Study

Materials ◽

10.3390/ma14237266 ◽

2021 ◽

Vol 14 (23) ◽

pp. 7266

Author(s):

Kamil P. Grela ◽

Dominik M. Marciniak ◽

Bożena Karolewicz

Keyword(s):

Controlled Release ◽

Drug Release ◽

Castor Oil ◽

Oil Content ◽

Poloxamer 407 ◽

Isopropyl Myristate ◽

Cellulose Membrane ◽

Oil In Water ◽

Injection Force ◽

Novel Drug

This article covers the design and evaluation of a novel drug vehicle: a thermosensitive, injectable, high-oil-content (50% w/w) emulgel providing a controlled release of lipophilic pharmaceuticals. Different vegetable (castor, canola, olive, peanut, grapeseed, linseed), mineral (paraffin) and semisynthetic (isopropyl myristate, oleic acid) oils were screened for ibuprofen (IBU) solubility and for their capacity for high-shear emulsification in a 17% (w/w) aqueous solution of poloxamer 407. Chosen emulgels were subject to a rheological evaluation, a syringeability test (TA.XT texture analyser; 2 mL syringe; 18 G, 20 G and 22 G needles) and a drug release study (48 h; cellulose membrane; 0.05 mol/L phosphate buffer at pH 7.4). Castor oil turned out to be an optimal component for IBU incorporation. Blank and drug-loaded castor oil emulgels were susceptible to administration via a syringe and needle, with the absolute injection force not exceeding 3 kg (29.4 N). The drug release test revealed dose-dependent, quasi-linear kinetics, with up to 44 h of controlled, steady, linear release. The results indicate the significant potential of high-oil-content, oil-in-water thermosensitive emulgel formulations as vehicles for the controlled release of lipophilic APIs.

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