Resveratrol (RES) is a polyphenolic compound which has shown beneficial pharmacological effects such as anti-inflammatory, antioxidant, and anti-cancer effects. However, poor aqueous solubility, bioavailability, and low stability are the major limitations to the clinical application of RES. Therefore, in the present study, chitosan (CS) coated PLGA nanoparticles of RES (CS-RES-PLGA NPs) was developed, characterized and its anticancer activity was evaluated in the H1299 lung carcinoma cell line. The effects of the increase in CS coating and cryoprotectant concentration on particle size, polydispersity index (PDI) and zeta potential (ZP) were determined. The particle size, PDI, ZP and entrapment efficiency of the optimized CS-RES-PLGA NPs were found to be 341.56 ± 7.90 nm, 0.117 ± 0.01, 26.88 ± 2.69 mV and 75.13% ± 1.02% respectively. The average particle size and ZP showed a steady increase with an increase in CS concentration. The increase in positive zeta potential is evident for higher CS concentrations. The effect of trehalose as cryoprotectant on average particle size was decreased significantly (p < 0.05) when it was increased from 1%−5% w/v. TEM and SEM showed uniform particle distribution with a smooth surface and spherical shape. The CS coating provides modulation of in vitro drug release and showed a sustained release pattern. The stability of RES loaded PLGA NPs was improved by CS coating. CS-coated NPs showed greater cytotoxicity and apoptotic activities compared to free RES. The CS coated NPs had a higher antioxidant effect than the free RES. Therefore, CS coated PLGA NPs could be a potential nanocarrier of RES to improve drug solubility, entrapment, sustain release, stability and therapeutic application.

Cancer is a life-threatening disease, contributing approximately 9.4 million deaths worldwide. To address this challenge, scientific researchers have investigated molecules that could act as speed-breakers for cancer. As an abiotic drug delivery system, liposomes can hold both hydrophilic and lipophilic drugs, which promote a controlled release, accumulate in the tumor microenvironment, and achieve elongated half-life with an enhanced safety profile. To further improve the safety and impair the off-target effect, the surface of liposomes could be modified in a way that is easily identified by cancer cells, promotes uptake, and facilitates angiogenesis. Integrins are overexpressed on cancer cells, which upon activation promote downstream cell signaling and eventually activate specific pathways, promoting cell growth, proliferation, and migration. RGD peptides are easily recognized by integrin over expressed cells. Just like a multistage rocket, ligand anchored liposomes can be selectively recognized by target cells, accumulate at the specific site, and finally, release the drug in a specific and desired way. This review highlights the role of integrin in cancer development, so gain more insights into the phenomenon of tumor initiation and survival. Since RGD is recognized by the integrin family, the fate of RGD has been demonstrated after its binding with the acceptor’s family. The role of RGD based liposomes in targeting various cancer cells is also highlighted in the paper.

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The aim of this study was to prepare and evaluate α-mangostin-loaded polymeric nanoparticle gel (α-MNG-PLGA) formulation to enhance α-mangostin delivery in an epidermal carcinoma. The poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) were developed using the emulsion–diffusion–evaporation technique with a 3-level 3-factor Box–Behnken design. The NPs were characterized and evaluated for particle size distribution, zeta potential (mV), drug release, and skin permeation. The formulated PLGA NPs were converted into a preformed carbopol gel base and were further evaluated for texture analysis, the cytotoxic effect of PLGA NPs against B16-F10 melanoma cells, and in vitro radical scavenging activity. The nanoscale particles were spherical, consistent, and average in size (168.06 ± 17.02 nm), with an entrapment efficiency (EE) of 84.26 ± 8.23% and a zeta potential of −25.3 ± 7.1 mV. Their drug release percentages in phosphate-buffered solution (PBS) at pH 7.4 and pH 6.5 were 87.07 ± 6.95% and 89.50 ± 9.50%, respectively. The release of α-MNG from NPs in vitro demonstrated that the biphasic release system, namely, immediate release in the initial phase, was accompanied by sustained drug release. The texture study of the developed α-MNG-PLGA NPs gel revealed its characteristics, including viscosity, hardness, consistency, and cohesiveness. The drug flux from α-MNG-PLGA NPs gel and α-MNG gel was 79.32 ± 7.91 and 16.88 ± 7.18 µg/cm2/h in 24 h, respectively. The confocal study showed that α-MNG-PLGA NPs penetrated up to 230.02 µm deep into the skin layer compared to 15.21 µm by dye solution. MTT assay and radical scavenging potential indicated that α-MNG-PLGA NPs gel had a significant cytotoxic effect and antioxidant effect compared to α-MNG gel (p < 0.05). Thus, using the developed α-MNG-PLGA in treating skin cancer could be a promising approach.

The present study aimed to formulate and optimize 2ME-loaded PMs (2ME-PMs) for enhancing the anticancer activity of 2ME in prostate cancer (PC). The 2ME-PMs were formulated using PEG-PLGA (PL), Tween 80 (TW80), and alpha-lipoic acid (ALA). The optimization was carried out using a Box-Behnken design with the PL, TW80, and ALA as the independent variables and particle size (PS) as the response. The formulation was optimized for the lowest possible PS, and the software suggested optimum formula with 100.282 mg, 2%, and 40 mg for PL, TW80, and ALA, respectively. The optimized PMs had spherical morphology with PS of 65.36 ± 2.2 nm, polydispersity index (PDI) of 0.273 ± 0.03, and entrapment efficiency of 65.23 ± 3.5%. The in vitro drug release was 76.3 ± 3.2% after 24 h. The cell line studies using PC-3 cells showed IC50 values of 18.75 and 54.41 µmol for 2ME-PM and 2ME, respectively. The estimation of tumor biomarkers was also carried out. The tumor biomarkers caspase-9 (17.38 ± 1.42 ng/mL), tumor protein P53 (p53) (1050.0 ± 40.9 pg/mL), nitric oxide (NO) (0.693 ± 0.03 pg/mL), interleukin-1β (IL-1β) (25.84 ± 2.23 pg/mL), nuclear factor kappa B (NF-kB) (0.719 ± 0.07 pg/mL), interleukin-6 (IL-6) (2.53 ± 0.16 folds), and cyclooxygenase-2 (COX-2) (3.04 ± 0.5 folds) were determined for 2ME-PMs and the results showed that these values changed significantly compared to those of 2ME. Overall, the results showed that the formulation of 2ME to 2ME-PMs enhances the anticancer effect. The exploration of the combined advantages of PEG, PLGA, ALA, and PMs in cancer therapy and the delivery of 2ME is the major importance of this research work. PEG reduces the elimination of 2ME, PLGA enhances 2ME loading, ALA has an inherent apoptotic effect, and PMs can efficiently target tumor cells.