TY - JOUR
T1 - Venlafaxine HCl Encapsulated in Niosome
T2 - Green and Eco-friendly Formulation for the Management of Pain
AU - Hashemi, Seyyed Mohammad Hassan
AU - Enayatifard, Reza
AU - Akbari, Jafar
AU - Saeedi, Majid
AU - Seyedabadi, Mohammad
AU - Morteza-Semnani, Katayoun
AU - Babaei, Amirhossein
AU - Asare-Addo, Kofi
AU - Nokhodchi, Ali
N1 - Funding Information:
This work was funded by the Elite Researcher Grant Committee of the National Institutes for Medical Research Development (NIMAD) in Tehran, Iran, with grant number [963560].
Funding Information:
The authors also would wish to express their sincere and special appreciation to the research council of Mazandaran University of Medical Sciences, Sari, Iran, for their valuable and technical cooperation.
Publisher Copyright:
© 2022, The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.
PY - 2022/7/1
Y1 - 2022/7/1
N2 - Abstract: The goal of this experimentation was to increase the cutaneous absorption of venlafaxine HCl (VFX) encapsulated in a niosome (venlasosme) produced by an ultrasonic approach. The impact of the cholesterol:surfactant (Chol:Surf) proportion was examined to modify the venlasosme properties. Photon correlation spectroscopy, powder X-ray diffraction (PXRD), SEM, DSC, and ATR-FTIR spectroscopy were utilized to investigate the solid-state and morphology of VFX in the venlasosme. The studies revealed that increasing the level of Chol in the venlasosme increased the size of the particles. Alterations in the Chol to surfactant ratios (when Chol decreased from 2.5 to 0%) caused the zeta potential enhancement from 7.37 ± 0.67 to 15.53 ± 1.47 mV. The venlasosme with the highest cholesterol concentration (2.5%) had the highest encapsulation efficiency (approximately 63%). PXRD results revealed that VFX in venlasosme was in the amorphous form. The levels of VFX in the cutaneous layers and the receiver compartment were higher for the venlasosme gel than for VFX simple gel in the cutaneous permeability study and showed no cutaneous irritancy in rats. Furthermore, the venlasosme gel demonstrated significant antinociceptive and anti-inflammatory responses when compared to the control groups (VFX simple gel and diclofenac gel). The topical administration of the venlasosme gel also considerably increased the tail-flick and hot-plate response time when compared to the VFX simple gel, control groups, and diclofenac gel (p < 0.05). These findings suggest that niosomes can improve VFX efficacy as an antinociceptive and anti-inflammatory substance by improving the medicaments delivery to the specified site.
AB - Abstract: The goal of this experimentation was to increase the cutaneous absorption of venlafaxine HCl (VFX) encapsulated in a niosome (venlasosme) produced by an ultrasonic approach. The impact of the cholesterol:surfactant (Chol:Surf) proportion was examined to modify the venlasosme properties. Photon correlation spectroscopy, powder X-ray diffraction (PXRD), SEM, DSC, and ATR-FTIR spectroscopy were utilized to investigate the solid-state and morphology of VFX in the venlasosme. The studies revealed that increasing the level of Chol in the venlasosme increased the size of the particles. Alterations in the Chol to surfactant ratios (when Chol decreased from 2.5 to 0%) caused the zeta potential enhancement from 7.37 ± 0.67 to 15.53 ± 1.47 mV. The venlasosme with the highest cholesterol concentration (2.5%) had the highest encapsulation efficiency (approximately 63%). PXRD results revealed that VFX in venlasosme was in the amorphous form. The levels of VFX in the cutaneous layers and the receiver compartment were higher for the venlasosme gel than for VFX simple gel in the cutaneous permeability study and showed no cutaneous irritancy in rats. Furthermore, the venlasosme gel demonstrated significant antinociceptive and anti-inflammatory responses when compared to the control groups (VFX simple gel and diclofenac gel). The topical administration of the venlasosme gel also considerably increased the tail-flick and hot-plate response time when compared to the VFX simple gel, control groups, and diclofenac gel (p < 0.05). These findings suggest that niosomes can improve VFX efficacy as an antinociceptive and anti-inflammatory substance by improving the medicaments delivery to the specified site.
KW - anti-inflammatory effect
KW - antinociceptive
KW - niosomes
KW - topical
KW - venlafaxine HCl
UR - http://www.scopus.com/inward/record.url?scp=85130366826&partnerID=8YFLogxK
U2 - 10.1208/s12249-022-02299-5
DO - 10.1208/s12249-022-02299-5
M3 - Article
C2 - 35595933
AN - SCOPUS:85130366826
VL - 23
JO - AAPS PharmSciTech
JF - AAPS PharmSciTech
SN - 1530-9932
IS - 5
M1 - 149
ER -