Nano-transfersomal formulations for transdermal delivery of asenapine maleate: <i>in vitro</i> and <i>in vivo</i> performance evaluations

Shreya, Ajjappla Basavaraj; Managuli, Renuka S.; Menon, Jyothsna; Kondapalli, Lavanya; Hegde, Aswathi R.; Avadhani, Kiran; Shetty, Pallavi K.; Amirthalingam, Muthukumar; Kalthur, Guruprasad; Mutalik, Srinivas

doi:10.3109/08982104.2015.1098659

Cited by 65 publications

(30 citation statements)

References 32 publications

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“…These results were in agreement with our previous findings where nanoparticles (containing morin), transferosomes (containing asenapine and epigallocatechin‐3‐gallate [EGCG]) exhibited higher retention within the skin for the corresponding drugs . Enhanced skin permeation and a consequent increased deposition within the skin can be ascribed to the enhanced passage of NPs through corneocytes and the lipid matrix (transcellular route) and the shunt pathway (transappendageal route) .…”

Section: Resultssupporting

confidence: 92%

Sunscreen creams containing naringenin nanoparticles: Formulation development and in vitro and in vivo evaluations

Joshi

Hegde

Shetty

et al. 2017

Photoderm Photoimm Photomed

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Section: Resultssupporting

confidence: 92%

Sunscreen creams containing naringenin nanoparticles: Formulation development and in vitro and in vivo evaluations

Joshi

Hegde

Shetty

et al. 2017

Photoderm Photoimm Photomed

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“…To the best of our knowledge, just one paper has been published on SNP chiral separation, but using CE with unmodified β‐cyclodextrin and without biological application . On the other hand, some analytical methods have been published for the non‐enantioselective determination of SNP in biological matrices among which those designed for patient monitoring are very few and only one dealing with micromatrices . None of them was applied to real samples from psychiatric patients, nor have they compared different and novel dried microsampling approaches.…”

Section: Introductionmentioning

confidence: 99%

Enantioseparation and determination of asenapine in biological fluid micromatrices by HPLC with diode array detection

Protti

Vignali

Blanco

et al. 2018

J of Separation Science

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Asenapine is a recent drug approved in the European Union for the treatment of bipolar disorder. An original approach has been developed for asenapine analysis in patients treated with the drug, including miniaturized microsampling procedures, separation and quantitation of drug enantiomers. An original enantioselective method based on high-performance liquid chromatography with diode array detection was developed and applied to the determination of asenapine enantiomer levels in innovative haematic samples: four micromatrices have been tested, two based on dried matrix spots (dried blood spots and dried plasma spots) and two based on volumetric absorptive microsampling (from blood and plasma). Chiral separation was achieved on a cellulose-tris(3,5 dimethylphenylcarbamate) column, with a mobile phase containing bicarbonate buffer and acetonitrile. The method was validated with satisfactory results of linearity and precision on all matrices that showed also a significant performance in terms of stability, feasibility and reliability, when compared to fluid plasma sampling, handling and processing. Among micromatrices, both volumetric absorptive microsampling types were superior to dried matrix spots in terms of data reproducibility and correspondence with plasma levels. The bioanalytical approach proposed herein provides for the first time a chiral high-performance liquid chromatographic method for the determination of asenapine enantiomers, coupled to a very effective microsampling strategy.

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“…It has been proven that it serves as an alternative approach to avoid the first-pass metabolism of drugs and improve bioavailability in peroral delivery. [23] Even though several research works are being carried out to enhance the solubility and bioavailability of AM by formulating it as sublingual tablets, fast mouth dissolving film, [24] nanostructured lipid carriers for intranasal delivery, [25] nano-transfersomal formulations for transdermal delivery, [26] and in situ nasal gel, [27] still it is required to design the oral formulation having combined advantages such as sustained release and avoiding first-pass metabolism of AM using peroral route of delivery. Therefore, the aim of the present work was to improve the oral bioavailability of AM by formulating it as SLN.…”

Section: Resultsmentioning

confidence: 99%

Untitled

Gambhire¹

2018

AJP

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Introduction: The aim of the present research work was to develop asenapine maleate (AM)-loaded solid lipid nanoparticles (AM-SLN) for the enhancement of oral bioavailability of drug and delivery to the brain. Materials and Methods: A 3 2 factorial design was used for the development and optimization of AM-SLN. Two independent variables, drug:lipid ratio (X 1) and number of homogenization cycles (X 2), were selected, while particle size and entrapment efficiency were selected as response variables. The optimized batch was evaluated by various in vitro characterizations and in vivo pharmacokinetic and brain distribution studies. Results: The particle size, polydispersity index, entrapment efficiency, and zeta potential of optimized AM-SLN were found to be 113 ± 4 nm, 0.34 ± 0.05, 72.4 ± 1.73%, and −41.4 ± 2.25 mV, respectively. Pharmacokinetic study indicated significantly higher (P < 0.05) peak drug concentration (142.41 ± 8.14 ng/mL), area under the drug concentrationtime curve (1561.81 ± 36.34 h ng/mL), and mean residence time (15.31 ± 3.21 h) of AM-SLN compared to AM-suspension (77.02 ± 5.74 ng/mL, 299.76 ± 39.42 ng/mL, and 2.73 ± 0.16 h, respectively) through oral route. Brain distribution study showed higher drug permeation across the blood-brain barriers and accumulation in the brain. Conclusion: These findings demonstrate that SLNs could be a new promising drug delivery system for oral delivery of AM in the treatment of schizophrenia.

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Nano-transfersomal formulations for transdermal delivery of asenapine maleate: in vitro and in vivo performance evaluations

Abstract: Dual strategy of permeation enhancement was successful in increasing the transdermal permeation and bioavailability of ASPM.

Cited by 65 publications

References 32 publications

Sunscreen creams containing naringenin nanoparticles: Formulation development and in vitro and in vivo evaluations

Sunscreen creams containing naringenin nanoparticles: Formulation development and in vitro and in vivo evaluations

Enantioseparation and determination of asenapine in biological fluid micromatrices by HPLC with diode array detection

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