Paliperidone-Loaded Mucoadhesive Microemulsion in Treatment of Schizophrenia: Formulation Consideration

Patel, Rashmin B.; Patel, Mrunali R.; Bhatt, Kashayap K.; Patel, Bankim

doi:10.1007/s12247-013-9160-3

Cited by 20 publications

(28 citation statements)

References 24 publications

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“…Water was added dropwise to each oilEmix mixture under vigorous stirring. After equilibrium, the samples were visually checked and determined as being clear/transparent (Elshafeey et al 2009;Jogani et al 2008;Kumar et al 2008;Patel et al 2009Patel et al , 2013a.…”

Section: Construction Of Phase Diagrammentioning

confidence: 99%

“…The globule size was calculated using Stokes-Einstein relationship by Zetasizer Software. Electrophoretic mobility (lm/s) was measured using small volume disposable zeta cell and converted to zeta potential by in-built software using Helmholtz-Smoluchowski equation (Elshafeey et al 2009;Jogani et al 2008;Kumar et al 2008;Patel et al 2009Patel et al , 2013a.…”

Section: Globule Size and Zeta Potentialmentioning

confidence: 99%

“…The major problem in treating mental disorders is due to the inability of the therapeutic agents to surpass the blood brain barrier (BBB) and the blood cerebrospinal fluid barrier. One of the possibilities to overcome this barrier is drug delivery to brain using novel drug delivery systems like nanoemulsions exploring nanotechnology (Canuso et al 2008;Patel et al 2010Patel et al , 2013aPatel et al , b, 2014.…”

Section: Introductionmentioning

confidence: 99%

“…Paliperidone (PALI) is an atypical antipsychotic agent that belongs to the class of benz-isoxazole and approved for the treatment of schizophrenia (Canuso et al 2008;Patel et al 2010Patel et al , 2013aPatel et al , b, 2014. It is a lipophilic drug having oral bioavailabity of 28 %.…”

Section: Introductionmentioning

confidence: 99%

“…The olfactory region of the nasal mucosa provides a direct connection between the nose and the brain. The advantages of nasal route are rapid absorption; higher bioavailability reduced first pass metabolism, non-invasive administration, and selfmedication as well as improved patient compliance (Canuso et al 2008;Patel et al 2013aPatel et al , b, 2014. It is also reported in our earlier studies that absorption of PALI through transnasal route was more efficient when given in an oil based formulation (microemulsion) (Patel et al 2013a, b).…”

Section: Introductionmentioning

confidence: 99%

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Preparation and in vitro/ex vivo evaluation of nanoemulsion for transnasal delivery of paliperidone

Patel¹,

Patel²,

Patel³

2016

Appl Nanosci

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Paliperidone was formulated in mucoadhesive nanoemulsion with the aim of improving its solubility and transnasal delivery, which can further utilized for its preclinical evaluation. Solubility of Paliperidone in oils, emulsifiers, co-emulsifiers was determined to identify nanoemulsion components. Emulsifier and co-emulsifiers were screened for their ability to emulsify selected oily phase. Phase diagrams were constructed to identify the area of nanoemulsification. Paliperidone nanoemulsion was formulated using spontaneous nanoemulsification method. The three nanoemulsions (PMNE4, PMNE5, and PMNE6) containing 5.71-6.80 % oleic acid as an oily phase, 47.62-51.63 % labrasol and plurol oleique CC 497 as emulsifier mixture (1:1), 42.86-45.58 % (wt/wt) aqueous phase having a suitable optical transparency of 98.33-99.33 %, globule size of 28.8-43.2 nm and polydispersity of 0.129-0.152 were selected for the incorporation of mucoadhesive polymer. The PMNE6 showed highest flux (5.072 ± 0.13 lg/cm 2 /min) with enhancement ratio of 1.1 as compared to Paliperidone solution (PS). The diffusion co-efficient of PMNE6 was significantly higher than PMNE5, PMNE4 and PS and followed higuchi model. The formulation was found to be free from nasal cilio toxicity. All formulations were found to be stable for 6 months at room temperature.

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