Microemulsion based intranasal delivery system for treatment of insomnia

Porecha, sheetal K; Shah, Tapan; Jogani, Viral; Naik, Sachin; Misra, Ambikanandan

doi:10.1080/10717540802560381

Cited by 26 publications

(27 citation statements)

References 20 publications

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“…480 (blood) following intranasal administration. Reports in the literature reveal that the drug uptake into the brain from the nasal mucosa mainly occurs via three different pathways (Vyas et al, 2006;Jogani et al, 2008;Porecha et al, 2009). One is the systemic pathway by which some of the drug is absorbed into the systemic circulation and subsequently reaches the brain by crossing BBB.…”

Section: Bio-distribution Studiesmentioning

confidence: 99%

“…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%

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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: Bio-distribution Studiesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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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“…The retention is due to the electronic interaction between mucin of nasal mucosa and the polymer (Rhee et al, 2007). Evidences of intranasal drug delivery systems formulated using mucoadhesive agent and its benefits in enhancing nose-to-brain drug transport have been reported by various scientists in the literature (Porecha et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Mucoadhesive microemulsion of ibuprofen: design and evaluation for brain targeting efficiency through intranasal route

Mandal

Chuttani

et al. 2015

Braz. J. Pharm. Sci.

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This study aimed at designing mucoadhesive microemulsion gel to enhance the brain uptake of Ibuprofen through intranasal route. Ibuprofen loaded mucoadhesive microemulsion (MMEI) was developed by incorporating polycarbophil as mucoadhesive polymer into Capmul MCM based optimal microemulsion (MEI) and was subjected to characterization, stability, mucoadhesion and naso-ciliotoxicity study. Brain uptake of ibuprofen via nasal route was studied by performing biodistribution study in Swiss albino rats. MEI was found to be transparent, stable and non ciliotoxic with 66.29 ± 4.15 nm, -20.9 ± 3.98 mV and 98.66 ± 1.01% as average globule size, zeta potential and drug content respectively. Transmission Electron Microscopy (TEM) study revealed the narrow globule size distribution of MEI. Following single intranasal administration of MMEI and MEI at a dose of 2.86 mg/kg, uptake of ibuprofen in the olfactory bulb was around 3.0 and 1.7 folds compared with intravenous injection of ibuprofen solution (IDS). The ratios of AUC in brain tissues to that in plasma obtained after nasal administration of MMEI were significantly higher than those after intravenous administration of IDS. Findings of the present investigation revealed that the developed mucoadhesive microemulsion gel could be a promising approach for brain targeting of ibuprofen through intranasal route.Uniterms: Ibuprofen/brain-targeting. Ibuprofen/intranasal administration. Ibuprofen/mucoadhesion. Mucoadhesive microemulsion gel. Drugs/design. Transmission electron microscopy.O objetivo deste trabalho foi planejar microemulsão/mucoaesiva em gel a fim de melhorar a captação cerebral de ibuprofeno por via intranasal. A microemulsão para mucoadesão com ibuprofeno (MMEI) foi desenvolvida pela incorporação de policarbofil como polímero mucoadesivo em microemulsão otimizada (MEI) com base em Capmul (MCM) e foi submetida à caracterização, estabilidade, mucoadesão e naso-ciliotoxicidade. A captação cerebral de ibuprofeno pela via nasal foi estudada por meio de estudo de biodistribuição em ratos albinos suíços. MEI se mostrou transparente, estável e não ciliotóxica, com 66,29 ± 4,15 nm, -20,9 ± 3,98 mV e 98,66 ± 1,01%, respectivamente, de tamanho médio dos glóbulos, potencial zeta e conteúdo do fármaco. O estudo revelou o estreita distribuição do tamanho dos glóbulos de MEI. Após administração intranasal única de MMEI e MEI, em dose de 2,86 mg/kg, a captação de ibuprofeno no bulbo olfativo foi em torno de 3,0 e 1,7 vezes maior, comparativamente, à injeção endovenosa de ibuprofeno (IDS). As taxas de ASC em tecido cerebral em relação ao plasma, obtidas após administração da MMEI nasal, foram, significativamente, mais elevadas do que aquelas observadas após a administração intravenosa de IDS. Os resultados do presente estudo mostraram que a microemulsão/mucoadesiva em gel poderia ser uma abordagem promissora para o direcionamento cerebral de ibuprofeno por via intranasal.Unitermos: Ibuprofeno/captação cerebral. Ibuprofeno/administração intranasal. Ibuprofeno/mucoadesão. Microemuls...

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“…Nasal route has advantages of rapid absorption of drug, higher bioavailability allowing lower doses, fast onset of therapeutic action, avoidance of liver or gastrointestinal metabolism, avoidance of irritation of the gastrointestinal membrane, reduced risk of overdose, non-invasive administration, ease of convenience and self-medication and improved patient compliance (Li et al, 2002;Vyas et al, 2006b;Jogani et al, 2008;Kaur & Kim, 2008;Elshafeey et al, 2009;Patel et al, 2013b). Researchers are making many attempts to find efficient and new way to prevent extensive first-pass metabolism and target the drug to the receptor site in brain for treating brain disorders (Chow et al, 1999;Li et al, 2002;Zhang et al, 2004;Vyas et al, 2005;Vyas et al, 2006a,b;Jogani et al, 2008;Kaur & Kim, 2008;Kumar et al, 2008a,b;Porecha et al, 2009;Sharma et al, 2009;Patel, 2013b).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of brain targeting efficiency of intranasal microemulsion containing olanzapine: pharmacodynamic and pharmacokinetic consideration

Patel¹,

Patel

Bhatt

et al. 2014

Drug Delivery

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The objective of this study was to develop and evaluate olanzapine (OZP) -loaded microemulsions (OZPME) for intranasal delivery in the treatment of schizophrenia. The OZPME was formulated by the spontaneous microemulsification method and characterized for physicochemical parameters. Pharmacodynamic assessments (apomorphine -induced compulsive behavior and spontaneous locomotor activity) were performed using mice. All formulations were radiolabeled with technetium-99 ( 99m Tc), and biodistribution of drug in the brain was investigated using Swiss albino rats. Brain scintigraphy imaging in rabbits was performed to determine the uptake of the OZP into the brain. OZPME were found clear and stable with average globule size of 23.87 ± 1.07 nm. In pharmacodynamic assessments, significant (p50.05) difference in parameters estimated were found between the treated and control groups.99m Tc-labeled OZP solution (OZPS)/OZPME/OZP mucoadhesive microemulsion (OZPMME) were found to be stable and suitable for in vivo studies. Brain/blood ratio at all sampling points up to 8 h following intranasal administration of OZPMME compared to intravenous OZPME was found to be five to six times higher signifying larger extent of distribution of the OZP in brain. Drug targeting efficiency and direct drug transport were found to be highest for intranasal OZPMME, compared to intravenous OZPME. Furthermore, rabbit brain scintigraphy also demonstrated higher intranasal uptake of the OZP into the brain. This investigation demonstrates a prompt and larger extent of transport of OZP into the brain through intranasal OZPMME, which may prove beneficial for treatment of schizophrenia.

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Microemulsion based intranasal delivery system for treatment of insomnia

Cited by 26 publications

References 20 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

Mucoadhesive microemulsion of ibuprofen: design and evaluation for brain targeting efficiency through intranasal route

Evaluation of brain targeting efficiency of intranasal microemulsion containing olanzapine: pharmacodynamic and pharmacokinetic consideration

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