Preparation of Encapsulated Resveratrol Liposome Thermosensitive Gel and Evaluation of Its Capability to Repair Sciatic Nerve Injury in Rats

Abstract

The purpose of this study was to prepare a liposomal temperature-sensitive gel able to slowly release resveratrol after local intramuscular injection. The best formulation of resveratrol liposomes was based on the highest encapsulation efficiency and drug loading designed by Box-Behnken. The prepared liposomes were approximately circular, with a mean particle diameter of 161.5±0.12 nm and zeta potential of -6.9 mV. The optimized liposomes were dispersed in a polymer gel (PLGA-PEG-PLGA) for preparation of an in situ-formed gel at 35±2°C. In vitro release of the prepared liposome temperature-sensitive gel was studied and compared with ordinary drug-releasing gels, revealing a significantly longer drug release time. Finally, a rat sciatic nerve injury model was used to evaluate the pharmacological activity of the liposome temperature-sensitive gels for the repair of damaged nerves. The results indicate that the gel was able to promote recovery of damaged nerves.

Development, Optimization, and In Vitro Evaluation of Novel Oral Long-Acting Resveratrol Nanocomposite In-Situ Gelling Film in the Treatment of Colorectal Cancer

“…Resveratrol (3,5,4-trihydroxytrans-stilbene [Rv]) is a polyphenolic compound extracted from red grapes seeds that showed various pharmacological activities, such as anticancer and antioxidant and anti-inflammatory properties [ 1 , 2 ]. Rv has free radical scavenging activity to achieve its cancer-protective effects [ 1 , 2 , 3 ]. Regarding Rv’s effects on gene expression, Rv induces activation of caspases-3 and -9 and enhancement of B-cell lymphocyte-associated protein X (Bax) and tumor protein 53 (P53) expression to trigger apoptosis of cancerous cells [ 4 , 5 ].…”

“…On the other hand, Rv presents several disadvantages, such as low bioavailability, high metabolism, and instability. High Rv metabolism, especially after oral ingestion, decreases its oral bioavailability and increases the need for repetitive administration, and is associated with Rv adverse effects and diminished patient adherence and compliance [ 1 , 2 , 3 , 8 , 10 ]. Additionally, Rv is prone to chemical and physical degradation during storage [ 4 ].…”

Resveratrol Loaded Liposomes Disrupt Cancer Associated Fibroblast Communications within the Tumor Microenvironment to Inhibit Colorectal Cancer Aggressiveness

“…The liposome solution (0.5 mL) was loaded into the dialysis bag with a molecular weight cut-off of 100 kDa. The solution was dialyzed against a PBS buffer, pH 7.4, with 1.5% TWEEN 80 (15 mL) at 37 °C, 180 rpm shaking [ 38 ]. One milliliter of PBS buffer was collected and replaced with equal volume at 0, 1, 2, 4, 6, 24, and 48 h during the dialysis process.…”

“…One milliliter of PBS buffer was collected and replaced with equal volume at 0, 1, 2, 4, 6, 24, and 48 h during the dialysis process. The concentration of RES in the collected medium was quantified using high-performance liquid chromatography (HPLC) following the protocol described elsewhere [ 38 ]. Briefly, the mixed solvent of methanol and water (65:35) was used as a mobile phase in a C18 column.…”

Design and Evaluation of Paeonol-Loaded Liposomes in Thermoreversible Gels for Atopic Dermatitis

“…It is easily absorbed after local administration and has good stability. However, poloxamers can form a hydrogel containing a large amount of water, which can cause a blasting reaction such that drugs are released in large quantities in the initial stage [ 39 ], preventing drugs from having a long-term therapeutic effect.…”