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. 2020 Oct 14:15:7937-7949.
doi: 10.2147/IJN.S268846. eCollection 2020.

In vitro Characterization and Release Studies of Combined Nonionic Surfactant-Based Vesicles for the Prolonged Delivery of an Immunosuppressant Model Drug

Akhtar Rasul #  1 , Muhammad Imran Khan #  2 , Mujeeb Ur Rehman #  1 , Ghulam Abbas #  1 , Nosheen Aslam #  3 , Shabbir Ahmad #  4 , Khizar Abbas #  5 , Pervaiz Akhtar Shah #  6 , Muhammad Iqbal #  7 , Ali Mohammad Ahmed Al Subari #  7 , Talal Shaheer #  8 , Shahid Shah #  9
Affiliations

In vitro Characterization and Release Studies of Combined Nonionic Surfactant-Based Vesicles for the Prolonged Delivery of an Immunosuppressant Model Drug

Akhtar Rasul et al. Int J Nanomedicine. .

Abstract

Background: Cyclosporine A (CsA) is an exceptional immunosuppressant used for the treatment of immune disorders. Niosomal vesicles are promising drug carriers that are formed by self-association of nonionic surfactants and cholesterol in an aqueous phase. The objective of the study was to formulate combined nonionic surfactant based vesicles and to evaluate their in vitro characterization, release studies and in vivo studies.

Materials and methods: Five niosomal formulations (F7 to F11) were prepared using the thin film hydration method. The molar ratio of cholesterol and non-ionic surfactant taken was 1:1. In formulation F10, the combination of surfactants Span 20 and Brij 35 was used. The niosomes were characterized by zeta sizer and SEM for particle size analysis, in vitro drug release and stability studies. The pharmacokinetic studies were conducted on healthy albino rabbits.

Results: The size of niosome was found in the range of 427.1 nm to 972.3 nm. SEM image of optimized formulations F10 exhibit the spherical nature of niosomal vesicles. DSC thermograms of niosomal formulations exhibited a broadened endothermic peak. The stability study exhibited that all formulations are stable and negligible change of vesicle size and entrapment was observed with time. The percentage drug release was significantly higher as compared to CsA plain dispersion for all niosomal formulations at pH 1.2 and 7.4. The release kinetic behavior showed that all preparations were best described by zero order and can release active ingredient in a sustained manner. The pharmacokinetic data showed the test formulation (F10) possessed greater bioavailability as compared to the reference formulation (CsA aqueous dispersion).

Conclusion: The formulation F10 demonstrated a comparatively more delayed rate of release with enhanced dissolution as compared to a single surfactant scheme. The F10 formulation can be a remarkable nanotechnology for prolonged delivery of CsA orally with improved dissolution profile and bioavailability.

Keywords: cyclosporine A; in vitro study; niosomes; nonionic surfactants.

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Conflict of interest statement

The authors report no conflicts of interest for this work.

Figures

Figure 1
Figure 1
Solubility profile of CsA with nonionic surfactants at pH 1.2 and 7.4.
Figure 2
Figure 2
DSC thermograms of Span 20, Brij 35, physical mixture 3 (PM3), physical mixture 4 (PM4), F7, F8, F9, F10 and F11 formulations.
Figure 3
Figure 3
Size (A) and zeta potential (B) of niosomal formulations.
Figure 4
Figure 4
SEM appearance of optimized formulation F10.
Figure 5
Figure 5
EDX spectra of selected niosomal formulation F10.
Figure 6
Figure 6
Drug release profiles of formulations F7-F11 and drug aqueous suspension at pH 1.2.
Figure 7
Figure 7
Drug release profiles of formulations F7-F11 and drug aqueous suspension at pH 7.4.
Figure 8
Figure 8
Pharmacokinetic profile of F10 niosomal formulation and aqueous dispersion of CsA in healthy albino rabbits.
See this image and copyright information in PMC

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