Abstract
Propolis is a honeybee product that contains a mixture of natural substances with a broad spectrum of biological activities. However, the clinical application of propolis is limited due to the presence of a myriad of constituents with different physicochemical properties, low bioavailability and lack of appropriate formulations. In this study, a modified injection technique (spraying technique) has been developed for the encapsulation of the Egyptian propolis within liposomal formulation. The effects of three variables (lipid molar concentration, drug loading and cholesterol percentage) on the particle size and poly dispersity index (PDI) were studied using response surface methodology and the Box–Behnken design. Response surface diagrams were used to develop an optimized liposomal formulation of the Egyptian propolis. A comparative study between the optimized liposomal formulation prepared either by the typical ethanol injection method (TEIM) or the spraying method in terms of particle size, PDI and the in-vitro anti-proliferative effect against human melanoma cell line A375 was carried out. The spraying method resulted in the formation of smaller propolis-loaded liposomes compared to TEIM (particle sizes of 90 ± 6.2 nm, and 170 ± 14.7 nm, respectively). Furthermore, the IC50 values against A375 cells were found to be 3.04 ± 0.14, 4.5 ± 0.09, and 18.06 ± 0.75 for spray-prepared propolis liposomes (PP-Lip), TEIM PP-Lip, and propolis extract (PE), respectively. The encapsulation of PE into liposomes is expected to improve its cellular uptake by endocytosis. Moreover, smaller and more uniform liposomes obtained by spraying can be expected to achieve higher cellular uptake, as the ratio of liposomes or liposomal aggregates that fall above the capacity of cell membrane to “wrap” them will be minimized.
Highlights
Natural products have caught the attention of formulators to design a suitable dosage to maximize the therapeutic effects of these effective components
Propolis has a unique chemical composition as it is rich in polyphenolics, flavonoids, resins, balsams, waxes, amino acids and oils [3]
Many studies jave investigated the pharmacological activity of propolis [4,5,6,7,8,9], including its anticancer [10], antioxidant [11], antimicrobial [12], antiviral [13] and wound healing [14] properties, in addition to immunomodulatory effects [15]
Summary
Natural products have caught the attention of formulators to design a suitable dosage to maximize the therapeutic effects of these effective components. Many studies jave investigated the pharmacological activity of propolis [4,5,6,7,8,9], including its anticancer [10], antioxidant [11], antimicrobial [12], antiviral [13] and wound healing [14] properties, in addition to immunomodulatory effects [15]. Propolis has been reported to possess cytotoxic activity against different murine and human melanoma cell lines, including B16-F10 [16], B16-F1, and A375 [17]. Propolis has an expansive therapeutic potential, its processing and formulation development are strictly hindered due to its resinous and sticky consistency, low solubility, and physical instability [18]
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