Pluronic gels for nasal delivery of Vitamin B12. Part I: Preformulation study

Pisal, Sambhaji S.; Paradkar, Anant; Mahadik, Kakasaheb R.; Kadam, Shivajirao

doi:10.1016/j.ijpharm.2003.10.005

Cited by 96 publications

(45 citation statements)

References 29 publications

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“…The dispersion was stored in a refrigerator at 2-4°C overnight for effective dissolution of Pluronic F127. The next day, active ingredient flurbiprofen was dissolved in lecithin-isopropyl palmitate solution directly or first in polyethylene glycol-600 (Pisal et al, 2004) and then mixed with the lecithin-isopropyl palmitate solution (polyethylene glycol-600 acts as a co-solvent as well as moisturizer). Finally, 70% aqueous phase was slowly added in 30% oil phase with stirring at 400 rpm using a mechanical stirrer.…”

Section: Methods Of Preparationmentioning

confidence: 99%

Pluronic lecithin organogel as a topical drug delivery system

et al. 2009

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Section: Methods Of Preparationmentioning

confidence: 99%

Pluronic lecithin organogel as a topical drug delivery system

et al. 2009

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“…Progesterone nanoparticles might be localized within the micelles core so they did not affect water content of the gel, micellar aggregation, or the gelling temperature. 32 It is clear that all the bases except B2 will be able to congeal inside the body at physiological temperature. In most of the studied bases, the gelation temperature is far below the body temperature.…”

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confidence: 99%

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Salem¹

2010

IJN

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Abstract:The production of an intramuscular (IM) injection of natural progesterone would provide a safer solution than using semi synthetic progesterone. However, disadvantages such as low solubility and a short half life prevent the use of natural progesterone. In this study, we formulated a sustained release form of natural progesterone to be given as IM injection. A progesterone nanosuspension (PNS) was first developed and then dispersed in a thermosensitive gel matrix. The selected nanoparticles showed an average particle size of 267 nm and a zeta potential approaching-41 mV. The in vitro release profile of PNS from the F127 plus methyl cellulose gel followed zero order kinetics and correlated linearly with the weight percentage of gel dissolved, demonstrating that the overall rate of release of PNS is controlled by dissolution of the pluronic F127/methyl cellulose (MC) gel (r 2 . 0.99). The pharmacokinetic parameters of the PNS (6 mg/mL) in pluronic F127/MC gel were evaluated in comparison with the control progesterone suspension. After the administration of PNS in F127/MC gel into the rats, a maximum serum concentration of 22.1 ± 1.9 ng/mL was reached at a T max of 4.05 ± 0.1 h. The terminal half life was 12.7 ± 0.8 h. The area under the curve AUC 0-∞ of the injected formula was 452.75 ± 42.8 ng·h/mL and the total mean residence time was 18.57 ± 1.44 h. The PNS in gel was significantly different from the control in rate and extent at P , 0.001. The natural progesterone which was nanosized and formulated in a thermosensitive gel significantly sustained the action of natural progesterone so that it could be injected every 36 h instead of every day. Moreover, this formula is expected to provide a much safer choice than the use of semi-synthetic progesterone.

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“…57 . On the basis of 13 C NMR studies Pisal 58 suggested that at high temperature, conformational changes in the methyl group of the polyoxypropylene within the hydrophilic micellar region and in the motion of the hydrophilic end chains takes place. This results in dehydration and end chain friction, which causes the gelation.…”

Section: Rheological Behaviourmentioning

confidence: 99%

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine

Lungare

Bowen

Badhan

2016

Journal of Pharmaceutical Sciences

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The aim of this study was to develop and characterise an intranasal delivery system for amantadine (AMT). Optimal formulations (F) consisted of a thermosensitive polymer Pluronic ® 127 (P127) and either carboxy methyl cellulose (CMC) or chitosan (CS) which demonstrated gel-transition at nasal cavity temperatures (34 °C ± 1 °C). Rheologically, the loss tangent (Tan δ) confirmed a three-stage gelation phenomena at 34 °C ± 1 °C and nonNewtonian behaviour. Storage of FCMC and FCS at 4 °C for 8 weeks resulted in repeatable release profiles at 34 °C when sampled, with a Fickian mechanism earlier on but moving towards anomalous transport by week 8. Polymers (P127, CMC and CS) demonstrated no significant cellular toxicity to human nasal epithelial cells up to 4 mg/mL and up to 1 mM for AMT (IC50: 4.5 mM ± 0.05 mM). FCMC and FCS demonstrated slower release across an in-vitro human nasal airway model (43-44 % vs 79 % ± 4.58 % for AMT). Using a human nasal cast model, deposition into the olfactory regions (potential nose-to-brain) was demonstrated upon nozzle insertion (5 mm) whereas tilting of the head forward (15°) resulted in greater deposition in the bulk of the nasal cavity. KEYWORDSParkinson's disease; rheology; nasal; RPMI 2650; nose to brain; thermoresponsive; 3 INTRODUCTION Parkinson's disease (PD) is an ageing associated progressive neurological disorder and affects 1.5 % of the population over 65-years of age 1 , with age-adjusted prevalence rates thought to be around 150 per 100,000 with a suggested mean onset in the 70's 1 . Ageing is the largest single risk factor for the development of PD and the pathogenesis of PD is composed of a range of events leading towards neuronal apoptosis, primarily of degradation of dopamine neurones in the sustantia nigra. The mainstay of clinical drug therapy focuses on increases the levels of dopamine (DA) in the brain, with oral dosing of levodopa being the most commonly used to pharmacological intervention treatment to reverse the symptoms of PD. It is also common to use adjunct therapies in conjunction with levodopa, such as the weak NMDA-type receptor antagonist amantadine, which can aid in blocking dopamine reuptake.

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Pluronic gels for nasal delivery of Vitamin B12. Part I: Preformulation study

Cited by 96 publications

References 29 publications

Pluronic lecithin organogel as a topical drug delivery system

Pluronic lecithin organogel as a topical drug delivery system

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine

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