Formulation and Evaluation of Azithromycin-Loaded Niosomal Gel: Optimization, In Vitro Studies, Rheological Characterization, and Cytotoxicity Study

Abstract

Several novel, innovative approaches for improving transdermal delivery of BCS class III drugs have been proposed. Despite their great aqueous solubility, BCS class III drugs have the drawback of limited permeability. The objective of the current work was to screen the suitability of niosomes as a nanocarrier in permeation enhancement of azithromycin (AZM) transdermal delivery. Niosomes were prepared by an ether injection method using a nonionic surfactant (Span 60) and cholesterol at different concentrations. The ζ potential (ZP), polydispersity index (PDI), and particle size (PS) of AZM-loaded niosomes were evaluated. The size of the niosomes was found to vary between 288 and 394 nm. The results revealed that the niosomes prepared in a ratio of 2:1 (Span 60: cholesterol) had larger vesicle sizes, but all of them were characterized by narrow size distributions (PDI <0.95). Niosomal gel was successfully prepared using different polymers. The appearance, pH, viscosity, and ex vivo drug release of niosomal gel formulations were all examined. The flow curves showed that the niosomal gel displayed lower viscosity values than its corresponding conventional gels. Niosomal and conventional gels exhibited a domination of the elastic modulus (G′) over the viscous modulus (G″) (G’>G″) in the investigated frequency range (0.1–100 rad/s), indicating stable gels with more solid-like properties. Ex vivo skin permeation studies for the niosomal gel show 90.83 ± 3.19% of drug release in 24 h as compared with the conventional gel showing significantly lower (P < 0.001) drug release in the same duration (1.25 ± 0.12%). Overall, these results indicate that niosomal gel could be an effective transdermal nanocarrier for enhancing the permeability of AZM, a BCS class III drug. In conclusion, this study suggests that transdermal formulations of AZM in the niosomal gel were successfully developed and could be used as an alternative route of administration.

Preparation and Characterization of Patch Loaded with Clarithromycin Nanovesicles for Transdermal Drug Delivery

“…Based on these findings, the niosomal formulation maintained the antimicrobial activity of the CLR without affecting the effective concentration. This result agreed with the study in [ 32 ], which showed that niosomes containing azithromycin exhibited an antibacterial activity against S. aureus and S. epidermidis that was comparable to that of free azithromycin.…”

“…A cytotoxicity assay for the CLR niosomal patches (P4) and the blank niosomal patches was performed according to the MTT cytotoxicity assay as described in [ 32 ]. Briefly, MCF-7 cells were seeded in 96-well plates at concentrations of 5000 cells/well and cultured in the presence of either a CLR transdermal patch (P4) or a blank patch (without CLR).…”

Qbd-Based Approach to Optimize Niosomal Gel of Levosulpiride for Transdermal Drug Delivery

“…These results were also consistent with the earlier studies reported [ 38 , 39 ], which show that increasing the cholesterol amount, makes the membrane more rigid hence reducing the effect of sonication and can produce large-size niosomes. It is also described in the literature that the cholesterol changes the fluidity of the chains in the bilayers and hence the breadth of the lipid layer which in turn leads to large niosomes [ 40 ]. On the other hand, the amount of Span 40 (X 2 ) and sonication time (X 3 ) demonstrated a negative effect on the size of prepared niosomes and were significant ( p < 0.001).…”

Composite polymeric microsponge‐based long‐acting gel formulation for topical delivery of mupirocin

“…The estimation was performed in triplicate and represented as an average with standard deviation. 13,20 The drug content was calculated by the following formula 8 :…”

“…In a medical setting, the infection site should have a sufficient supply of antimicrobial medication for the required time. 5,6 Multiple attempts with different strategies have been explored to date for prolonged topical drug delivery, and in most of the studies drug release up to 24 h is evaluated to ensure the effectiveness of the developed formulation [7][8][9] Gel formulation containing carrier like microsponges is one of the promising approach for controlled topical drug delivery. 10 Gel-based formulations are generally preferred over creams and ointments as gels are of light texture, non-sticky, water-based, possess good hydration ability, and are easily washable.…”