A novel drug delivery system of mixed micelles based on poly(ethylene glycol)‐poly(lactide) and poly(ethylene glycol)‐poly(ɛ‐caprolactone) for gambogenic acid

Abstract

In this study, a novel mixed polymeric micelles formed from biocompatible polymers, poly(ethylene glycol)‐poly(lactide) (mPEG‐PLA) and poly(ethylene glycol)‐poly(ɛ‐caprolactone) (mPEG‐PCL), used as a novel nanocarrier to encapsulate gambogenic acid (GNA). GNA‐loaded mixed polymeric micelles (GNA‐MMs) was prepared by cosolvent evaporation method. The mean average size of GNA‐MMs was (83.23 ± 1.06) nm (n = 3) and entrapment efficiency (EE%) of GNA‐MMs was (90.18 ± 2.59) % (n = 3) as well as (12.36 ± 0.64) % (n = 3) for drug loading (DL%). Transmission electron microscopy revealed that the GNA‐MMs were spherical with “core‐shell” structures. Compared with free GNA solution, in vitro release of GNA from GNA‐MMs showed a two‐phase sustained release profile: an initial relatively fast phase and followed by a slower release phase. Pharmacokinetic results also indicated that the GNA‐MMs have longer systemic circulation time and slower plasma elimination rate than free GNA solution. Moreover, the in vitro cytotoxicity assay showed that the IC50 values on HepG2 cells for GNA‐MMs and free GNA were (5.67 ± 0.02) μM and (9.02 ± 0.03) μM, respectively. In addition, GNA‐MMs significantly increased the HepG2 cellular apoptosis in a concentration‐dependent manner. In conclusion, the results showed that mPEG‐PLA/mPEG‐PCL mixed micelles may serve as an ideal drug delivery system for GNA to prolong drug circulation time in body, enhance bioavailability and retained its potent antitumor effect.

Imperatorin-Loaded RH60/mPEG–PLLA Micelles for Reversing Tamoxifen Resistance in Breast Cancer

“…Notably, the mixed micelles have the lowest CMC, which provides good stability for the drugs and prevents dissociation and precipitation in blood due to dilution. 17,41 The IMP-RH60/mPEG−PLLA, prepared by a solvent evaporation method, has a drug loading capacity of 2.66 ± 0.03% and a particle size of 25.48 ± 0.92 nm, which enhances its permeability and cellular uptake. 40,42 Consequently, IMP-RH60/mPEG−PLLA demonstrates cellular uptake capability and enhanced bioavailability.…”

“…The CMC of mPEG–PLLA, RH60, and RH60/PM mixed systems are determined to be 15.81, 5.75, and 4.64 μg/mL, respectively. Notably, the mixed micelles have the lowest CMC, which provides good stability for the drugs and prevents dissociation and precipitation in blood due to dilution. , …”

Oral Delivery of Gambogenic Acid by Functional Polydopamine Nanoparticles for Targeted Tumor Therapy

“…Lin prepared GNA-loaded mixed polymeric micelles to enhance the bioavailability of GNA, but it failed to achieve controlled and targeted release of the drug by oral administration. 12 Herein, we proposed modified functional polydopamine nanoparticles (PDA NPs) as an effective stabilizer and delivery system for GNA to both improve water solubility of GNA and achieve tumor targeting via oral administration. PDA, known as a water-insoluble biopolymer, was synthesized by the oxidation of dopamine (DA) under weak alkaline conditions (pH ∼ 8.5).…”

“…Meanwhile, oral drug delivery is highly dependent on the water solubility of the drug. Lin prepared GNA-loaded mixed polymeric micelles to enhance the bioavailability of GNA, but it failed to achieve controlled and targeted release of the drug by oral administration …”

Influence of Solvent and Substrate on Hydrophobicity of PLA Films

“…Polylactic acid (PLA) is a biopolymer widely used nowadays in various applications [1]: medical devices [2,3], prostheses [4,5], food packaging [6,7], drug delivery systems [8,9], 3D printing [10,11], supports [12], shape memory materials [13], etc. Due to its use in the biomedical field, not only the study of its mechanical and surface properties is of great importance, but also the evaluation of its ability to deal with bacterial activity and to promote cell growth and proliferation.…”