Development of phenytoin intranasal microemulsion for treatment of epilepsy

Acharya, Sheetal Porecha; Pundarikakshudu, Kilambi; Upadhyay, Pratik; Shelat, Pragna K.; Lalwani, Anita

doi:10.1007/s40005-015-0190-3

Cited by 16 publications

(16 citation statements)

References 12 publications

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“…In addition to that, intranasal drug delivery enables reduction in the dose, quick therapeutic level attainment of the drug into the blood, speedier onset of pharmacological activity, and fewer side effects ( Arora et al, 2002 , Ugwoke et al, 2001 ). It is reported that lipophilic drugs are by and large, well absorbed from the nasal cavity with pharmacokinetic profiles, which are frequently indistinguishable to those acquired after an intravenous infusion with a bioavailability approaching 100% ( Aacharya et al, 2015 ). Strategy of delivering the drug by intranasal route could be effective in the delivery of therapeutic proteins such as brain delivered neurotropic factor (BDNF) to the olfactory bulb as a treatment for Alzheimer’s disease ( Thorne et al, 1995 ).…”

Section: Introductionmentioning

confidence: 99%

Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent to the brain through nasal route

Upadhyay

Trivedi

Pundarikakshudu

et al. 2017

Saudi Pharmaceutical Journal

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The problem of inadequate oral bioavailability of Quetiapine Fumarate, a lipophilic drug used for schizophrenia, due to hepatic metabolism and repulsion by brain barrier was attempted in this study. Combination of two approaches, viz. Quetiapine inclusion into the liposomal carrier for better diffusion and administration through nasal route to avoid hepatic metabolism and barrier elimination was applied. Thin film hydration followed by sonication method was employed in liposome preparation and the formulation was optimized using 3 full factorial design. The number of sonication cycles () of 2 min and 80% amplitude and molar ratio of constructional components such as cholesterol to egg phosphatidylcholine () as independent variables and a % of entrapment efficiency () and cumulative drug release () at 6 h as dependent variables was selected. Batch F7 prepared by 2 cycles of sonication and 1:3 M ratio of cholesterol:egg phosphatidylcholine was optimized as a consequence of substantial entrapment efficiency of 75.63 ± 3.77%, and 99.92 ± 1.88% drug release and 32.33 ± 1.53% drug diffusion, which was optimum among all other batches at 6 h. Diffusion study was done for all the batches of liposomal formulation by using sheep nasal mucosa and good amount with better diffusion rate was measured which proved liposomal dispersion a virtuous delivery system for brain drug delivery through nasal route. Results of , ciliotoxicity and gamma scintigraphy studies on mice supported the above inference.

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Section: Introductionmentioning

confidence: 99%

Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent to the brain through nasal route

Upadhyay

Trivedi

Pundarikakshudu

et al. 2017

Saudi Pharmaceutical Journal

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“…Measured volume of distilled water was added dropwise to the above mixture and vortexed to obtain transparent microemulsion. 20,21 The composition of microemulsions was showed in Table 1.…”

Section: Preparation Methods Microemulsionsmentioning

confidence: 99%

Formulation and Characterization of Amisulpride Microemulsions for Brain Targeting via Intranasal Route-Pharmacodynamic Evaluation in Rat Model

Ganta¹,

Velupula²,

Janapareddi³

2020

JYP

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Amisulpride was gifted by Dr. Reddy's (Hyderabad, India). Labrasol, Transcutol P, lauroglycol 90, capmul MCM were received as gift samples from Gattefosse Company (Mumbai, India). Polyethylene glycol 400 (PEG 400), Polysorbate 80, Oleic acid, coconut oil, Tween 20, Propylene glycol, potassium chloride, Oleic acid, Arachis oil, sodium hydroxide, potassium dihydrogen orthophosphate, potassium chloride were purchased from SD fine chem Ltd (Mumbai, India) are of analytical grade. Methanol and Acetonitrile were purchased from Merck Limited (Mumbai, India). All other chemicals were analytical grade and purchased commercially. Double distilled water was used throughout the study.

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“…Ex vivo drug diffusion study was carried out using freshly obtained sheep nasal mucosal epithelium from slaughter house (Arumugam et al, 2008;Jung et al, 2009;Acharya et al, 2015;Lohan et al, 2015). Mucosal membrane (0.2 mm thick, 10 mm diameter and 78.5 mm 2 area) was fixed in between receptor and donor compartment of the Franz diffusion cell.…”

Section: Ex Vivo % Drug Diffusion (%Dd)mentioning

confidence: 99%

“…Although various strategies have been applied to attain brain delivery of QTF, still requires further improvement (Kararli et al, 1992;Lohan et al, 2015). Several studies reported that lipophilic drugs are generally well absorbed from the nasal route with pharmacokinetic profiles (Ding et al, 2007), which are frequently indistinguishable to those acquired after an intravenous infusion with a bioavailability approaching 100% (Acharya et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

Comparative study between simple and optimized liposomal dispersion of quetiapine fumarate for diffusion through nasal route

et al. 2015

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Context: Nasal route of drug administration is preferred more and more for the targeted delivery to the brain in current drug development scenario due to its ease of use, reliability, quick action, and lesser side effects. Those CNS drugs which have limited oral bioavailability due to pharmacokinetic consequences and brain barrier repulsion are getting onto this direction. Objective: Quetiapine fumarate, an analogous to above and an antischizophrenic agent, is tested for its diffusion property with and without lipophilic carrier through sheep nasal membrane. Being a BCS class II' and high permeable candidate, it tends to crossover easily, so made up in a simple dispersion. Materials and methods: To improve its diffusion rate, it was embedded into liposomal dispersion, which has proven that it has advanced efficiency for diffusion. For this, both the formulations were checked and compared for their diffusion profile, as it is an essential property for bioavailability through nasal route. Comparison was made on the basis of % drug diffusion within 6 h, rate, mechanism, profile, and coefficient. Results: Liposomal dispersion has been proved superior with greater percentage diffusion of 32.61 ± 1.70 and very high permeability with a coefficient value of 4.1334 ± 0.7321 (Â 10 À 5 cm/s). Diffusion profile comparison bearing dissimilarity of 18 and similarity of 74 indicated that the diffusion profiles of liposomal dispersions and simple dispersion were similar but not identical. Conclusion: Liposomal diffusion supremacy was further sustained by in vivo, ciliotoxicity, and gamma scintigraphy studies.

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Development of phenytoin intranasal microemulsion for treatment of epilepsy

Cited by 16 publications

References 12 publications

Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent to the brain through nasal route

Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent to the brain through nasal route

Formulation and Characterization of Amisulpride Microemulsions for Brain Targeting via Intranasal Route-Pharmacodynamic Evaluation in Rat Model

Comparative study between simple and optimized liposomal dispersion of quetiapine fumarate for diffusion through nasal route

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