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. 2022 Feb 18;8(2):129.
doi: 10.3390/gels8020129.

Tacrolimus-Loaded Solid Lipid Nanoparticle Gel: Formulation Development and In Vitro Assessment for Topical Applications

Abdul Shakur Khan  1 , Kifayat Ullah Shah  1 , Mohammed Al Mohaini  2   3 , Abdulkhaliq J Alsalman  4 , Maitham A Al Hawaj  5 , Yousef N Alhashem  6 , Shakira Ghazanfar  7 , Kamran Ahmad Khan  1 , Zahid Rasul Niazi  1 , Arshad Farid  8
Affiliations

Tacrolimus-Loaded Solid Lipid Nanoparticle Gel: Formulation Development and In Vitro Assessment for Topical Applications

Abdul Shakur Khan et al. Gels. .

Abstract

The currently available topical formulations of tacrolimus have minimal and variable absorption, elevated mean disposition half-life, and skin irritation effects resulting in patient noncompliance. In our study, we fabricated tacrolimus-loaded solid lipid nanoparticles (SLNs) that were converted into a gel for improved topical applications. The SLNs were prepared using a solvent evaporation method and characterized for their physicochemical properties. The particle size of the SLNs was in the range of 439 nm to 669 nm with a PDI of ≤0.4, indicating a monodispersed system. The Zeta potential of uncoated SLNs (F1-F5) ranged from -25.80 to -15.40 mV. Those values reverted to positive values for chitosan-decorated formulation (F6). The drug content and entrapment efficiency ranged between 0.86 ± 0.03 and 0.91 ± 0.03 mg/mL and 68.95 ± 0.03 and 83.68 ± 0.04%, respectively. The pH values of 5.45 to 5.53 depict their compatibility for skin application. The surface tension of the SLNs decreased with increasing surfactant concentration that could increase the adherence of the SLNs to the skin. The release of drug from gel formulations was significantly retarded in comparison to their corresponding SLN counterparts (p ≤ 0.05). Both SLNs and their corresponding gel achieved the same level of drug permeation, but the retention of the drug was significantly improved with the conversion of SLNs into their corresponding gel formulation (p ≤ 0.05) due to its higher bioadhesive properties.

Keywords: chitosan; gel; solid lipid nanoparticles; tacrolimus; topical drug delivery.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Morphology of optimized SLN formulations using TEM analysis.
Figure 2
Figure 2
Particle size distribution of optimized SLN formulations using DLS analysis.
Figure 3
Figure 3
Drug release pattern from (A) SLN formulations and (B) SLN-loaded gel.
Figure 4
Figure 4
Permeation of drug through the skin from (A) SLNs formulation and (B) SLN-loaded gel.
Figure 5
Figure 5
Drug retention profile in the skin from (A) SLN formulations and (B) SLN-loaded gel.
See this image and copyright information in PMC

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