The present research work describes development of dual drug‐loaded lipid–polymer hybrid nanoparticles (LPHNPs) of anticancer therapeutics for the management of colon cancer. The epidermal growth factor (EGF)‐functionalized LPHNPs coloaded with 5‐fluorouracil (FU) and sulforaphane (SFN) were prepared by one‐step nanoprecipitation method. Box–Behnken design was applied for optimizing the material attributes and process parameters. The optimized LPHNPs revealed particle size 198 nm, polydispersity index 0.3, zeta potential
−25.3 mV, and drug loading efficiency 19–20.3% for 5‐FU and SFN, respectively. EGF functionalization on LPHNPs was confirmed from positive magnitude of zeta potential to 21.3 mV as compared with the plain LPHNPs. In vitro drug release performance indicated sustained and non‐Fickian mechanism release nature of the drugs from LPHNPs. Anticancer activity evaluation in HCT‐15 colon cancer cells showed significant reduction (p < 0.001) in the cell growth and cytotoxicity of the investigated drugs from various treatments in the order: EGF‐functionalized LPHNPs > plain LPHNPs > free drug suspensions. Overall, the research work corroborated improved treatment efficacy of EGF‐functionalized LPHNPs for delivering chemotherapeutic agents for the management of colon carcinoma.
With an increase in the global burden of cancer-related deaths, the quest for developing new therapeutic solutions has taken momentum. In this regard, the idea of using cancer vaccines came to existence approximately 30 years ago, where gene therapy interventions have shown significant improvement in the therapeutic outcomes against several types of cancers. Cancer vaccines usually encounter a number of challenges with limited targeting ability to the tumors. Nanocarriers have been studied as a technological innovation for tumor targeting of gene therapeutics. This article provides a critical insight into the recent progress made in nanotherapeutic strategies for genetic vaccine delivery for treatment against various types of cancers. Moreover, the article intends to provide a summary of the research work being done on this topic.
The present work
describes the development and characterization
of liquid crystalline nanoparticles of hispolon (HP-LCNPs) for treating
hepatocellular carcinoma. HP-LCNPs were prepared by a top-down method
utilizing GMO as the lipid and Pluronic F-127 as the polymeric stabilizer.
The prepared formulations (HP1–HP8) were tested for long-term
stability, where HP5 showed good stability with a particle size of
172.5 ± 0.3 nm, a polydispersity index (PDI) of 0.38 ± 0.31
nm, a zeta potential of −10.12 mV ± 0.05, an entrapment
efficiency of 86.81 ± 2.5%, and a drug loading capacity of 12.51
± 1.12%. Optical photomicrography and transmission electron microscopy
images demonstrated a consistent, low degree of aggregation and a
spherical shape of LCNPs. The effect of temperature and pH on the
optimized formulation (HP5) indicated good stability at 45 °C
and at pH between 2 and 5. In vitro gastrointestinal stability indicated
no significant change in the particle size, PDI, and entrapment efficiency
of the drug. The drug release study exhibited a biphasic pattern in
simulated gastric fluid (pH 1.2) for 2 h and simulated intestinal
fluid (pH 7.4) for up to 24 h, while the best fitting of the profile
was observed with the Higuchi model, indicating the Fickian diffusion
mechanism. The in vivo pharmacokinetic study demonstrated nearly 4.8-fold
higher bioavailability from HP5 (AUC: 1774.3 ± 0.41 μg*
h/mL) than from the HP suspension (AUC: 369.11 ± 0.11 μg*
h/mL). The anticancer activity evaluation revealed a significant improvement
in antioxidant parameters and serum hepatic biomarkers (SGOT, SGPT,
ALP, total bilirubin, and GGT) in the diethyl nitrosamine-treated
group of rats with the optimized LCNP formulation (HP5) vis-à-vis
HP suspension.
Long-acting preparations containing the antipsychotic paliperidone for intramuscular injection has drawn considerable attention to achieve harmless long-term treatment. This study aimed to develop paliperidone loaded polycaprolactone (PCL) nanoparticles and investigate the influence of PCL/drug ratio, stabilizer type, and chitosan coating on physicochemical properties, protein adsorption, and cellular toxicity. Results showed that chitosan coating produced enlarged particle sizes, shifted the surface charges from negative into positive and did not influence encapsulation efficiencies. Chitosan coating relatively sustained the drug release especially in pluronic stabilized formulations. Pluronic F127 based formulations exhibited the least protein adsorption (384.3 μg/mL). Chitosan coating of Tween 80 and polyvinyl alcohol stabilized formulations significantly (p < 0.05) increased protein adsorption. Cellular viability was concentration-dependent and negatively affected by stabilizers. All formulations did not show cellular death at 1.56 μg/mL. Inflammatory responses and oxidative stress were less affected by Tween 80 compared with other stabilizers. Chitosan minimized all aspects of cellular toxicity. Collectively, stabilizer type and chitosan coating play critical roles in developing safe and effective long-acting PCL nanoparticles intended for parenteral drug delivery. The coated formulations containing Tween 80 and Pluronic F127 as stabilizers are warranted a future in vivo study to delineate its safety and efficacy profiles.
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