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. 2021 May 29;26(11):3281.
doi: 10.3390/molecules26113281.

Formulation of Piperine-Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation

Syed Sarim Imam  1 , Sultan Alshehri  1 , Mohammad A Altamimi  1 , Afzal Hussain  1 , Wajhul Qamar  2 , Sadaf Jamal Gilani  3 , Ameeduzzafar Zafar  4 , Nabil K Alruwaili  4 , Saleh Alanazi  1 , Bjad K Almutairy  5
Affiliations

Formulation of Piperine-Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation

Syed Sarim Imam et al. Molecules. .

Abstract

The present research work is designed to prepare and evaluate piperine liposomes and piperine-chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (-7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

Keywords: MCF-7; breast cancer; chitosan; liposomes; mucoadhesive; piperine.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Vesicle size image of chitosan-coated PPN liposomes (PL3C1).
Figure 2
Figure 2
IR spectra of pure piperine, carriers and prepared chitosan-coated (PLF3C1) and uncoated liposomes (PLF3).
Figure 3
Figure 3
Surface morphology of (A). uncoated PPN liposomes (PLF3) and (B). chitosan-coated PPN liposomes (PLF3C1).
Figure 4
Figure 4
Comparative drug release study profile of pure PPN, PPN liposomes (PLF3) and chitosan-coated PPN liposomes (PLF3C1). The study was performed in triplicate and data are shown as mean ± SD.
Figure 5
Figure 5
Antioxidant activity of the tested samples using the DPPH method. The Tukey–Kramer multiple comparison test was utilized to analyze the statistically significant difference between each group. Difference was considered significant if p < 0.05. ns = not significant when compared between PPN liposomes (PLF3) and chitosan-coated PPN liposomes (PLF3C1); *** = p < 0.001 when compared with pure PPN; ** = p < 0.01 when compared with pure PPN.
Figure 6
Figure 6
Effect of different concentrations of pure PPN and LF3C1 on the viability of MCF7 cells evaluated by MTT assay. Data are presented in percent (%) in comparison to control as 100%. The Tukey–Kramer multiple comparison test was utilized to analyze the statistically significant difference between different concentration exposures and control. Difference was considered significant if p < 0.05. ns = not significant when compared with control; *** = p < 0.001 when compared with control; ### = p < 0.001 when compared with the same concentration groups of piperine standard.
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