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. 2020 Dec;27(1):888-899.
doi: 10.1080/10717544.2020.1775726.

Formulation and investigation of pilocarpine hydrochloride niosomal gels for the treatment of glaucoma: intraocular pressure measurement in white albino rabbits

Neelam Jain  1 , Anurag Verma  2 , Neeraj Jain  3
Affiliations

Formulation and investigation of pilocarpine hydrochloride niosomal gels for the treatment of glaucoma: intraocular pressure measurement in white albino rabbits

Neelam Jain et al. Drug Deliv. 2020 Dec.

Abstract

The present study was focused on investigating niosomal gels loaded with cholinergic drug; pilocarpine HCl, for prolonged precorneal residence time and improved bioavailability for glaucoma treatment. Pilocarpine HCl niosomes were prepared using various nonionic surfactants (span 20, span 60 and span 80), in the presence of cholesterol in different molar ratios by ether injection method. The selected formulations were incorporated into carbopol 934 and locust bean gum-based gels. TEM analysis confirmed that niosomes formed were spherical in shape and has a definite internal aqueous space with uniform particle size. Formulation F4 composed of span 60 and cholesterol (1:1) gave the highest entrapment (93.26 ± 1.75%) and slower release results after 8 hours (Q8h = 60.35 ± 1.87%) among other formulations. The in-vitro drug permeation studies showed that there was a prolonged release of drug from niosomal gels as compared to niosomes itself. Considering the in-vitro drug release, niosomal gel formulation G2 was the best among the studied formulations. The release data were fitted to an empirical equation, which indicated that the release follows non-Fickian diffusion mechanism. The stability study revealed that incorporation of niosomes in gel increased their stability than the niosome itself. No signs of redness, inflammation, swelling or increased tear production were observed over the study period for tested formulation by Draize's test. The intraocular pressure (IOP) lowering activity of G2 formulation showed relative bioavailability 2.64 times more than bioavailability of marketed Pilopine HS® gel. These results suggest that the niosomal gels containing pilocarpine HCl are promising ocular carriers for glaucoma treatment.

Keywords: Draize test; IOP; Niosomes; niosomal gel; pilocarpine HCl.

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Conflict of interest statement

The authors report no conflicts of interest.

Figures

Figure 1.
Figure 1.
Zeta potential of niosomal formulation.
Figure 2.
Figure 2.
Transmission electron micrograph of niosomal formulation at 30000X.
Figure 3.
Figure 3.
DSC thermogram tracings of pure drug.
Figure 4.
Figure 4.
DSC thermogram tracings of drug loaded niosomes.
Figure 5.
Figure 5.
In vitro release profile of different niosomal formulations.
Figure 6.
Figure 6.
Viscosity of niosomal gel formulations.
Figure 7.
Figure 7.
In vitro drug permeation of niosomal gels.
Figure 8.
Figure 8.
Comparative study for in-vitro drug release from niosome (F4) and niosomal gel (G2).
Figure 9.
Figure 9.
Stability studies of niosome formulation (F4) at different temperatures.
Figure 10.
Figure 10.
Stability studies of niosomal gel formulation (G2) at different temperatures.
Figure 11.
Figure 11.
Ex-vivo permeation study of selected formulation (G2) and marketed formulation.
Figure 12.
Figure 12.
Mean percentage decrease in intraocular pressure (% ΔIOP) versus time.
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