Propolis-Based Nanostructured Lipid Carriers for α-Mangostin Delivery: Formulation, Characterization, and In Vitro Antioxidant Activity Evaluation

Abstract

α-Mangostin (a xanthone derivative found in the pericarp of Garcinia mangostana L.) and propolis extract (which is rich in flavonoids and phenols) are known for their antioxidant properties, making them potential supplements for the treatment of oxidative stress-related conditions. However, these two potential substances have the same primary drawback, which is low solubility in water. The low water solubility of α-mangostin and propolis can be overcome by utilizing nanotechnology approaches. In this study, a propolis-based nanostructured lipid carrier (NLC) system was formulated to enhance the delivery of α-mangostin. The aim of this study was to characterize the formulation and investigate its influence on the antioxidant activity of α-mangostin. The results showed that both unloaded propolis-based NLC (NLC-P) and α-mangostin-loaded propolis-based NLC (NLC-P-α-M) had nanoscale particle sizes (72.7 ± 1.082 nm and 80.3 ± 1.015 nm, respectively), neutral surface zeta potential (ranging between +10 mV and −10 mV), and good particle size distribution (indicated by a polydispersity index of <0.3). The NLC-P-α-M exhibited good entrapment efficiency of 87.972 ± 0.246%. Dissolution testing indicated a ~13-fold increase in the solubility of α-mangostin compared to α-mangostin powder alone. The incorporation into the propolis-based NLC system correlated well with the enhanced antioxidant activity of α-mangostin (p < 0.01) compared to NLC-P and α-mangostin alone. Therefore, the modification of the delivery system by incorporating α-mangostin into the propolis-based NLC overcomes the physicochemical challenges of α-mangostin while enhancing its antioxidant effectiveness.

Alginate and Chitosan-Based Hydrogel Enhance Antibacterial Agent Activity on Topical Application

“…Interestingly, this dosage form is also compatible for the delivery of modified compounds on a nanoscale, such as curcumin loaded in β-cyclodextrin (curcumin-β-cyclodextrin complex). 64 , 89 , 90 The significant benefit of using alginate-chitosan-based hydrogel is evident from its testing as an antibacterial agent. Researchers have tested this hydrogel’s effectiveness against various types of bacteria, including S. aureus and P. aeruginosa.…”

Polymeric Nanohydrogel in Topical Drug Delivery System

“…NH can keep a lot of water without becoming mushy or losing their shape, despite their little size. 29 , 30 They offer several advantages for drug delivery such as, active ingredient protection, 31 , 32 biocompatibility, 7 , 33 versatile drug formulation, 13 , 33 stimuli-responsive properties, 34 preventing reticuloendothelial invasion, fast response to external stimuli, enhanced bioavailability. 33 Therefore, NH offer a range of advantages that make them promising candidates for drug delivery systems, particularly in topical therapy and targeted drug delivery applications.…”

“… 11 However, synthetic polymers lack immunological recognition for natural extracellular matrix proteins while offering great stability, maintaining the nanohydrogel structure, and well-behaved drug release qualities. 12 , 13 Several researchers have paired bioactive probes with synthetic polymers, while yet others have mixed bioactive probes with natural and synthetic polymers. 14 Numerous studies have focused on nanohydrogels, one of the most promising polymeric DDS, to investigate innovative formulation methodologies and uses of nanocarriers with enhanced therapeutic benefits.…”

Nanosuspension-Based Drug Delivery Systems for Topical Applications

“…The constrained solubility of these compounds poses a significant impediment during the initial phases of screening for pharmacological activity, as well as throughout the formulation development and clinical testing processes. 4 Preparing one of these substances for preclinical investigations and pharmacological activity assessments is a prerequisite well in advance of their commercialization. 5 Consequently, it becomes evident that the adoption of innovative technical strategies is imperative to augment the bioavailability of drugs characterized by low solubility.…”

“…A molecule can traverse the epidermis through one of two pathways: transcellularly, by passing through the corneocytes, or intercellularly, by moving through the lipid domains that separate the corneocytes. 4 , 32 Although it is generally accepted that the intercellular route serves as the primary pathway for drug penetration, this route is significantly restricted by the formidable barrier created by the outermost SC layer. 33 , 34 .…”