Intranasal delivery of gabapentin loaded optimized nanoemulsion for augmented permeation

Mallick, Archita; Gupta, Archita; Hussain, Afzal; Aparajay, Priyadarshi; Singh, Sneha; Singh, Sandeep Kumar; Dev, Abhimanyu

doi:10.1016/j.jddst.2020.101606

Cited by 15 publications

(7 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In agreement with the monolayer permeability results, BNEs demonstrated significantly higher brain disposition of BNN27 compared to the BNN27-loaded LIPs ( Figure 10 ). This result may be attributed to the previously reported effect of Capmul MCM to enhance drug permeability across the nasal mucosa and thus the brain disposition of drugs [ 21 , 43 ]. Furthermore, in vivo, the CHT-coating conferred enhanced brain concentrations of BNN27 for both formulation types (NEs and LIPs).…”

Section: Discussionmentioning

confidence: 65%

“…The higher amount of oil phase in the BNEs would also provide the capability to load higher amounts of BNN27. Furthermore, it was previously reported the Capmul improved the NE-loaded drug permeation through the BBB barrier [ 21 ].…”

Section: Resultsmentioning

confidence: 99%

“…In order to select the optimal materials, BNN27 solubility studies were carried out. The solubility of BNN27 was measured in three different oils that are commonly used in NEs [ 18 , 19 , 20 , 21 ], Capmul MCM, Labrafac Lipophile WL 1349, and Labrafac PG. Additionally three surfactants, Tween 20, Tween 80, and Cremophor EL RH40 as well as three co-surfactants, PEG 400, Transcutol HP, and a Transcutol HP/propylene glycol (1:1) mixture, were studied.…”

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Development and Comparative In Vitro and In Vivo Study of BNN27 Mucoadhesive Liposomes and Nanoemulsions for Nose-to-Brain Delivery

et al. 2023

View full text Add to dashboard Cite

Intranasal administration offers an alternative and promising approach for direct nose-to-brain delivery. Herein, we developed two chitosan (CHT)-coated (and uncoated) nanoformulations of BNN27 (a synthetic C-17-spiro-dehydroepiandrosterone analogue), liposomes (LIPs), and nanoemulsions (NEs), and compared their properties and brain disposition (in vitro and in vivo). LIPs were formulated by thin film hydration and coated with CHT by dropwise addition. BNN27-loaded NEs (BNEs) were developed by spontaneous emulsification and optimized for stability and mucoadhesive properties. Mucoadhesive properties were evaluated by mucin adherence. Negatively charged CHT-coated LIPs (with 0.1% CHT/lipid) demonstrated the highest coating efficiency and mucoadhesion. BNEs containing 10% w/w Capmul-MCM and 0.3% w/w CHT demonstrated the optimal properties. Transport of LIP or NE-associated rhodamine-lipid across the blood–brain barrier (in vitro) was significantly higher for NEs compared to LIPs, and the CHT coating demonstrated a negative effect on transport. However, the CHT-coated BNEs demonstrated higher and faster in vivo brain disposition following intranasal administration compared to CHT-LIPs. For both BNEs and LIPs, CHT-coating resulted in the increased (in vivo) brain disposition of BNN27. Current results prove that CHT-coated NEs consisting of compatible nasal administration ingredients succeeded in to delivering more BNN27 to the brain (and faster) compared to the CHT-coated LIPs.

show abstract

Section: Discussionmentioning

confidence: 65%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Development and Comparative In Vitro and In Vivo Study of BNN27 Mucoadhesive Liposomes and Nanoemulsions for Nose-to-Brain Delivery

et al. 2023

View full text Add to dashboard Cite

show abstract

“…To detect the nanoemulsion region and determine the component ratios for nanoemulsion formulation, a pseudo ternary phase diagram of oil, S-mix, and deionized water was developed using the aqueous titration method. 10 The weight ratios of surfactant/co-surfactant of S-mix screened for nanoemulsion formation were 1:1, 1:2, 1:3, 1:4, 2:1, 3:1, and 4:1. These ratios were used for a detailed study of phase diagram which reflects increasing concentrations of co-surfactant with respect to surfactant and increasing concentrations of surfactant concerning co-surfactant.…”

Section: Construction Of Pseudo Ternary Phase Diagrammentioning

confidence: 99%

Formulation and In-vitro Evaluation of Methotrexate Nanoemulsion using Natural Oil

Ashoor¹,

Ghareeb²

2022

IJDDT

View full text Add to dashboard Cite

Objective: The objective of the research was the preparation and evaluation of methotrexate nanoemulsion to improve its solubility, permeability, and bioavailability. Methods: The formulation components were selected based on the solubility study, and the pseudo-ternary phase diagrams were constructed by the aqueous phase titration method. Result and discussion: The prepared nanoemulsions were exposed to several thermodynamic stability studies and then to many characterizations tests for the selection of the best formulation. F 11 is the best formula since it has a 57 nm globule size, 0.21 polydispersity index, +23.67 zeta potential, and 99.57% light transmittance. FTIR study confirmed no incompatibility between drug and excipients. Conclusion: F 11 was a promising nanoemulsion formula that improved methotrexate permeability and bioavailability.

show abstract

“…Compositions of the co-loaded loratadine/sulpiride nanoemulsion formulations. For enhancing the image quality, 2% w/v phosphotungstic acid solution was added as a negative stained standard (Mallick et al, 2020). The morphology was also further confirmed via scanning electron microscope.…”

Section: Morphology Analysismentioning

confidence: 99%

A novel nasal co-loaded loratadine and sulpiride nanoemulsion with improved downregulation of TNF-α, TGF-β and IL-1 in rabbit models of ovalbumin-induced allergic rhinitis

et al. 2021

View full text Add to dashboard Cite

Purpose: The work aimed to develop a co-loaded loratadine and sulpiride nasal nanoemulsion for allergic rhinitis management. Methods: Compatibility studies were conducted adopting differential scanning calorimetry and Fourier transform infrared spectroscopy. Nanoemulsion formulations were prepared using soybean lecithin, olive oil and tween 80. Sodium cholate and glycerol were employed as co-surfactants. Nanoemulsions were assessed for viscosity, pH, droplet size, polydispersity index, zeta potential, electrical conductivity, entrapment, In vitro drug release and corresponding kinetics. Stability of the selected formulation was investigated. The biological effectiveness was evaluated in rabbit models of ovalbumin-induced allergic rhinitis by measuring TNF-a, TGF-b and IL-1. Results: Compatibility studies revealed absence of drug/drug interactions. Nanoemulsions exhibited > 90% entrapment efficiency. The selected nanoemulsion demonstrated small droplet size (85.2 ± 0.2 nm), low PDI (0.35 ± 0.0) and appropriate Zeta Potential (À23.3 ± 0.2) and stability. It also displayed enhanced in vitro drug release following the Higuashi Diffusion and Baker-Lonsdale models. The mean relative mRNA expression of TNF-a, IL-1 and TGF-b significantly decreased from 9.59 ± 1.06, 4.15 ± 0.02 and 4.15 ± 0.02 to 1.28 ± 0.02, 1.93 ± 0.06 and 1.56 ± 0.02 respectively after treatment with the selected nanoemulsion formulation. Conclusion: The results reflected a promising potent effect of the combined loratadine and sulpiride nasal nanoemulsion in managing the symptoms of allergic rhinitis.

show abstract

Intranasal delivery of gabapentin loaded optimized nanoemulsion for augmented permeation

Cited by 15 publications

References 27 publications

Development and Comparative In Vitro and In Vivo Study of BNN27 Mucoadhesive Liposomes and Nanoemulsions for Nose-to-Brain Delivery

Development and Comparative In Vitro and In Vivo Study of BNN27 Mucoadhesive Liposomes and Nanoemulsions for Nose-to-Brain Delivery

Formulation and In-vitro Evaluation of Methotrexate Nanoemulsion using Natural Oil

A novel nasal co-loaded loratadine and sulpiride nanoemulsion with improved downregulation of TNF-α, TGF-β and IL-1 in rabbit models of ovalbumin-induced allergic rhinitis

Contact Info

Product

Resources

About