Risperidone Microemulsion for Transnasal Delivery: Pharmacodynamic and Pharmacokinetic Evaluation

Patel, R. P.; Patel, Mrunali R.; Bhatt, Kashyap K.; Patel, Bankim; Mishra, Anil K.; Chutani, Krishna; Gaikwad, R. V.; Samad, Abdul

doi:10.2174/2211738511301010044

Cited by 15 publications

(53 citation statements)

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“…The mice were individually placed in glass containers of 250 mL capacity and the sign of stereotyped behavior, which include sniffing, rearing, licking and gnawing, were observed at 0, 15, 30, 45, 60 min after apomorphine administration. The intensity of stereotypy was recorded by the following scoring system (Shibuya & Nishimori, 1982;Kulkarni & Jisheph, 1998, Patel et al, 2013b.…”

Section: Apomorphine-induced Compulsive Behaviormentioning

confidence: 99%

“…First-generation antipsychotics are effective against psychosis but they do not improve and may even worsen the negative symptoms of schizophrenia and are linked with dose-limiting extrapyramidal symptoms (Patel et al, 2013b). Paliperidone (PALI) represents the second-generation most recent atypical antipsychotics which is chemically benzisoxazole derivative and commonly referred to as 9-hydroxyrisperidone.…”

Section: Introductionmentioning

confidence: 99%

“…Reportedly, nasal mucosal membrane offers a practical non-invasive route of administration for the therapeutic effect of many drugs (Li et al, 2002;Vyas et al, 2006;Jogani et al, 2008;Kaur & Kim, 2008;Elshafeey et al, 2009;Patel et al, 2013b). Nasal route has advantages of fast absorption of drug, enhanced bioavailability even at lower doses, rapid onset of therapeutic action, circumvent liver or gastrointestinal metabolism, reduced risk of overdose, non-invasive administration, convenient, self-medication and better patient compliance (Li et al, 2002;Vyas et al, 2006;Jogani et al, 2008;Kaur & Kim, 2008;Elshafeey et al, 2009;Patel et al, 2013b). Scientists are making many attempts to find efficient and new ways to prevent extensive first pass metabolism and target the drug to the receptor site in brain for treating brain disorders (Wolfgang & Heidrun, 2005;Porecha et al, 2009;Fazil et al, 2012;Md et al, 2013;Mahajan et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

“…The intranasal administration of drug can be increased by coadministering a permeation enhancer (Patel et al, 2013b). ME have been thoroughly studied as a drug carrier due to their special features, such as ease of preparation due to spontaneous formation, thermodynamic stability, high-solublization capacity for the hydrophilic and lipophilic drugs, transparent and elegant appearance, enhanced penetration through the biological membranes, increased bioavailability, and less inter-and intra-individual variability in drug pharmacokinetics (Li et al, 2002;Zhang et al, 2004;Wolfgang & Heidrun, 2005;Kaur & Kim, 2008;Elshafeey et al, 2009;Porecha et al, 2009;Shinde et al, 2011;Fazil et al, 2012;Md et al, 2013;Mahajan et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

“…Therefore it is essential to localize the formulation on a mucosal layer of nasal cavity to enhance drug absorption and prevent rapid nasal clearance. Addition of a well-designed muco-adhesive polymer to ME can prevent rapid nasal clearance of formulation (Patel et al, 2013b). This paper describes the development, characterization and pharmacodynamic-pharmacokinetic evaluation of PALI-loaded MME designed using Generally Regarded As Safe (GRAS) listed ingredients and polycarpophil AA-1 as a muco-adhesive component.…”

Section: Introductionmentioning

confidence: 99%

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Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation

Patel¹,

Patel²,

Bhatt³

et al. 2014

Drug Delivery

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Objective: The objective of present study was to develop and evaluate paliperidone (PALI) loaded microemulsion (PALI-ME) for intranasal delivery in the treatment of schizophrenia. Material and methods: The PALI-ME was formulated by the spontaneous microemulsification method and characterized for physicochemical parameters. Pharmacodynamic assessments (apomorphine-induced compulsive behavior and spontaneous motor activity) were performed using mice. All formulations were tagged with 99m Tc (technetium). Pharmacokinetic evaluation of PALI in the brain was investigated using Swiss albino rats. Brain scintigraphy imaging was performed in rabbits. Results and discussion: PALI-ME was found stable with average droplet size of 20.01 ± 1.28 nm. In pharmacodynamic studies, significant (p50.05) deference in parameters estimated, were found between the treated and control groups. Tc-tagged PALI solution (PALI-SOL)/ PALI-ME/PALI muco-adhesive ME (PALI-MME) was found to be stable and suitable for in vivo studies. Brain-to-blood ratio at all sampling points up to 8 h following intranasal administration of PALI-MME compared to intravenous PALI-ME was found to be 6-8 times higher signifying greater extent of distribution of the PALI in brain. Rabbit brain scintigraphy demonstrated higher intranasal uptake of the PALI into the brain. Conclusion: This investigation demonstrates a prompt and larger extent of transport of PALI into the brain through intranasal PALI-MME, which may prove beneficial for treatment of schizophrenia.

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Section: Apomorphine-induced Compulsive Behaviormentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation

Patel¹,

Patel²,

Bhatt³

et al. 2014

Drug Delivery

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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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Microemulsion for nasal delivery of Asenapine maleate in treatment of schizophrenia: formulation considerations

Patel

Hirani

Patel³

2017

J. Pharm. Investig.

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Risperidone Microemulsion for Transnasal Delivery: Pharmacodynamic and Pharmacokinetic Evaluation

Cited by 15 publications

References 0 publications

Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation

Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation

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

Microemulsion for nasal delivery of Asenapine maleate in treatment of schizophrenia: formulation considerations

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