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

Ganta, Abilash Teja; Velupula, Ravikrishna; Janapareddi, Krishnaveni

doi:10.5530/jyp.2020.12s.42

Cited by 3 publications

(1 citation statement)

References 16 publications

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“…The results of the experiments are presented as the mean SD of triplicate models, and the significance of the observed changes in the applied components was determined using one-way analysis of variance (ANOVA) at the 0.05 level of significance [36].…”

Section: Discussionmentioning

confidence: 99%

The Development of a Brain Targeted Mucoadhesive Amisulpride Loaded Nanostructured Lipid Carrier

TAMER

2023

FARMACIA

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This research aimed to create and refine intranasal mucoadhesive amisulpride-loaded nanostructured lipid carriers (AMS-MNLCs) to increase efficacy and safety by increasing nasal-mucosal adhesion and facilitating direct brain targetability. Using HPMC K4M, Carbopol 934, and Hyaluronic acid (HA), AMS-MNLCs were made by applying modified melt-emulsification and ultra-sonication procedures. The results of the pH, osmolarity, and mucoadhesive tests on the optimized formulation were 6.3 ± 0.02, 304.53 ± 2.15, and 26.07 ± 0.37, respectively. Rheological investigation, in-vitro release and ex-vivo permeation study of the optimized formulation revealed a shear-thinning behaviour, significantly higher release, and the flux of the drug from the formula was 975.2 ± 12.45. Based on the pharmacokinetic analyses in rats, intranasal AMS-MNLCs were reported to have a brain Cmax about 14 times higher than intravenous AMS-solution. In addition, two weeks of intranasal administration of formulation did not affect haematological parameters in the in vivo research. The histopathological investigation showed that there was no disruption of the naso-mucosal membrane structure. Therefore, the created and optimized intranasal MNLCs showed a promised venue for the efficient and secure delivery of AMS as an antiemetic drug for the prevention and treatment of preoperative nausea and vomiting (PONV). RezumatStudiul prezintă dezvoltarea unor nano-purtători lipidici mucoadezivi intranazali (AMS-MNLC) încărcați cu amisulprid, cu scopul creșterii eficacității și siguranței prin mărirea aderenței mucoasei nazale și facilitarea țintirii directe a creierului. Folosind HPMC K4M, Carbopol 934 și acid hialuronic (HA), purtătorii nanostructurați au fost obținuți prin proceduri modificate de emulsionare în topitură și ultrasunete. Rezultatele testelor de pH, osmolaritate și mucoadezivitate pentru formularea optimizată au fost 6,3 ± 0,02, 304,53 ± 2,15 și, respectiv, 26,07 ± 0,37. Investigația reologică, cedarea in vitro și studiul de permeație ex-vivo ale formulării optimizate au evidențiat un comportament de subțiere prin forfecare, eliberare semnificativ mai mare, iar fluxul medicamentului din formulă a fost de 975,2 ± 12,45. Pe baza analizelor farmacocinetice la șobolani, s-a observat că AMS-MNLC intranazal au o Cmax cerebrală de aproximativ 14 ori mai mare decât soluția intravenoasă de AMS. În plus, două săptămâni de administrare intranazală a formulării nu au afectat parametrii hematologici in vivo. Investigația histopatologică a arătat că nu a existat nici o perturbare a structurii membranei nazale. Prin urmare, purtătorii nanolipidici cu administrare intranazală obținuți au permis o cedare eficientă a AMS, folosit ca medicament antiemetic pentru prevenirea și tratamentul sindromului de greață și vomă preoperatorie (PONV).

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Section: Discussionmentioning

confidence: 99%

The Development of a Brain Targeted Mucoadhesive Amisulpride Loaded Nanostructured Lipid Carrier

TAMER

2023

FARMACIA

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Applications of innovative technologies to the delivery of antipsychotics

Bergonzi

Bilia

Landucci

2022

Drug Discovery Today

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Formulation, Optimization and Evaluation of amisulpride-loaded Niosomal Intranasal Gel for Brain Targeting

Patil,

Sutar,

Pockle

et al. 2023

Ther. Deliv.

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Aim: To develop stable non-ionic surfactant vesicles containing amisulpride (AMS) to improve brain uptake via nose to brain mechanism. Methods: Niosomes were developed using a modified ethanol injection technique, optimized using 32factorial design and evaluated for the vesicle size (VS), percent encapsulation efficiency (EE), zeta potential (ZP) and % cumulative drug release (%CDR). Results: Optimized niosomes (Span-60: cholesterol ratio 0:1) showed 191.4 nm VS, 84.25% EE, -38.2 ZP and 81.31% CDR. In situ gel with these niosomes displayed 78% CDR. TEM analysis revealed spherical niosomes. Pharmacokinetic and brain tissue distribution studies in rats showed enhanced plasma and brain concentrations, indicating successful brain targeting. Conclusion: This strategy demonstrates improved AMS permeation via the nasal cavity, enhancing bioavailability for treating schizophrenia.

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

Cited by 3 publications

References 16 publications

The Development of a Brain Targeted Mucoadhesive Amisulpride Loaded Nanostructured Lipid Carrier

The Development of a Brain Targeted Mucoadhesive Amisulpride Loaded Nanostructured Lipid Carrier

Applications of innovative technologies to the delivery of antipsychotics

Formulation, Optimization and Evaluation of amisulpride-loaded Niosomal Intranasal Gel for Brain Targeting

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