Anticancer Drug Delivery System Research Articles

Biomedical Polyurethanes for Anti-Cancer Drug Delivery Systems: A Brief, Comprehensive Review.

With the intensive development of polymeric biomaterials in recent years, research using drug delivery systems (DDSs) has become an essential strategy for cancer therapy. Various DDSs are expected to have more advantages in anti-neoplastic effects, including easy preparation, high pharmacology efficiency, low toxicity, tumor-targeting ability, and high drug-controlled release. Polyurethanes (PUs) are a very important kind of polymers widely used in medicine, pharmacy, and biomaterial engineering. Biodegradable and non-biodegradable PUs are a significant group of these biomaterials. PUs can be synthesized by adequately selecting building blocks (a polyol, a di- or multi-isocyanate, and a chain extender) with suitable physicochemical and biological properties for applications in anti-cancer DDSs technology. Currently, there are few comprehensive reports on a summary of polyurethane DDSs (PU-DDSs) applied for tumor therapy. This study reviewed state-of-the-art PUs designed for anti-cancer PU-DDSs. We studied successful applications and prospects for further development of effective methods for obtaining PUs as biomaterials for oncology.

An Emergent Role for Mitochondrial Bioenergetics in the Action of Snake Venom Toxins on Cancer Cells.

Beyond the role of mitochondria in apoptosis initiation/execution, some mitochondrial adaptations support the metastasis and chemoresistance of cancer cells. This highlights mitochondria as a promising target for new anticancer strategies. Emergent evidence suggests that some snake venom toxins, both proteins with enzymatic and non-enzymatic activities, act on the mitochondrial metabolism of cancer cells, exhibiting unique and novel mechanisms that are not yet fully understood. Currently, six toxin classes (L-amino acid oxidases, thrombin-like enzymes, secreted phospholipases A2, three-finger toxins, cysteine-rich secreted proteins, and snake C-type lectin) that alter the mitochondrial bioenergetics have been described. These toxins act through Complex IV activity inhibition, OXPHOS uncoupling, ROS-mediated permeabilization of inner mitochondrial membrane (IMM), IMM reorganization by cardiolipin interaction, and mitochondrial fragmentation with selective migrastatic and cytotoxic effects on cancer cells. Notably, selective internalization and direct action of snake venom toxins on tumor mitochondria can be mediated by cell surface proteins overexpressed in cancer cells (e.g. nucleolin and heparan sulfate proteoglycans) or facilitated by the elevated Δψm of cancer cells compared to that non-tumor cells. In this latter case, selective mitochondrial accumulation, in a Δψm-dependent manner, of compounds linked to cationic snake peptides may be explored as a new anti-cancer drug delivery system. This review analyzes the effect of snake venom toxins on mitochondrial bioenergetics of cancer cells, whose mechanisms of action may offer the opportunity to develop new anticancer drugs based on toxin scaffolds.

Biopolymeric nanoparticles based effective delivery of bioactive compounds toward the sustainable development of anticancerous therapeutics.

Nowadays, effective cancer therapy is a global concern, and recent advances in nanomedicine are crucial. Cancer is one of the major fatal diseases and a leading cause of death globally. Nanotechnology provides rapidly evolving delivery systems in science for treating diseases in a site-specific manner using natural bioactive compounds, which are gaining widespread attention. Nanotechnology combined with bioactives is a very appealing and relatively new area in cancer treatment. Natural bioactive compounds have the potential to be employed as a chemotherapeutic agent in the treatment of cancer, in addition to their nutritional benefits. Alginate, pullulan, cellulose, polylactic acid, chitosan, and other biopolymers have been effectively used in the delivery of therapeutics to a specific site. Because of their biodegradability, biopolymeric nanoparticles (BNPs) have received a lot of attention in the development of new anticancer drug delivery systems. Biopolymer-based nanoparticle systems can be made in a variety of ways. These systems have developed as a cost-effective and environmentally friendly solution to boost treatment efficacy. Effective drug delivery systems with improved availability, increased selectivity, and lower toxicity are needed. Recent research findings and current knowledge on the use of BNPs in the administration of bioactive chemicals in cancer therapy are summarized in this review.

Stimuli-responsive vitamin E-based micelles: Effective drug carriers with a controlled anticancer drug release

Herein, a series of vitamin E-based TPGS-poly(2-(dimethylamino)ethyl methacrylate)- b -poly(3-vinyl benzaldehyde) block copolymer micelles were synthesized via reversible addition−fragmentation chain-transfer polymerization (RAFT). d -α-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS) is a good candidate to overcome the big problem of multidrug resistance in cancer therapy because TPGS can inhibit permeability of glycoprotein (P-gp) resulting in restored sensitivity to chemotherapeutics. Doxorubicin (DOX) was loaded within the micelles, as an anticancer model drug, via hydrolytic amide linkage in the hydrophobic block. The DOX-loaded micelles demonstrated high potential as anticancer drug delivery systems through the release of the drug under acidic conditions, varying from pH 7.4 to 5.0. Three different micelles compositions were investigated with various ratios of hydrophilic and hydrophobic blocks (1:1, 4:3, and 4:1). The DOX-conjugated polymer with the shortest hydrophobic segment (4:1), TPGS-poly(2-(dimethylamino)ethyl methacrylate) 125 - b -poly(3-vinyl benzaldehyde) 91 , demonstrated excellent in vitro cytotoxicity with pH-responsive characteristics in comparison to free DOX. Although the higher degree of polymerization of the hydrophobic block promoted the drug loading efficiency of the micelles these compositions demonstrated lower cytotoxicity to the A549 cell line of human lung adenocarcinoma. It was concluded that the prepared pH-responsive micelles based on TPGS are promising drug carriers for anticancer drug delivery systems and could be considered to provide multi-drug resistance cancer treatments after further in vitro biological studies. • A series of block copolymers containing vitamin E moieties were synthesized. • Micelles with hydrophobic core and hydrophilic shell were loaded with DOX. • In vitro loading and release studies of DOX were performed. • Biocompatibility of vitamin E based micelles on healthy human cells was shown. • Obtained pH-responsive micelles appeared to be promising drug carriers.

Rational design of ibuprofen-based redox-responsive anti-cancer polymeric drug delivery systems

Rational design of ibuprofen-based redox-responsive anti-cancer polymeric drug delivery systems

β-cyclodextrin/alginate nanoparticles encapsulated 5-fluorouracil as an effective and safe anticancer drug delivery system

Although 5-Fluorouracil (5-FU) is one of the most frequently used cytotoxic chemotherapy drugs in the treatment of cancer, it possesses a short biological half-life and toxic side effects against normal healthy cells. In this work, β-cyclodextrin/alginate (β-CD/Alg) nanoparticles loaded with 5-fluorouracil (5-FU) were prepared to evaluate release properties and bioactivity in different pH media. Stable nanocomposites with the best loading efficiency (36%) and encapsulation efficiency (90%) were successfully fabricated. The size of the nanocomposite solution was determined via dynamic light scattering (DLS) to be in the range 30–120 nm with a mean size of 70 nm, while TEM images showed the particle size of the nanocomposite to be in the range 30–80 nm with a mean size of 50 nm. The release profile of 5-FU in a simulated gastric fluid (pH 1.2) was much lower than in a simulated colorectal fluid (pH 7.4). The release behaviour of 5-FU from the nanocomposite was confirmed by the change in morphology in the pH media. A cytotoxicity assay indicated that the nanocomposite is an effective delivery system for 5-FU with strong antiproliferative activity against MCF-7 cells and negligible effects on normal healthy cells.

Manufacturing and characterizing of the poly (ε-caprolactone)/poly (N-vinyl-2-pyrrolidone) core-shell nanofibers loaded by multi-walled carbon nanotubes coated by polypyrrole via vapor phase and chemical method and its application as an electro-responsive anticancer drug delivery system

The drug release systems are useful in controlling efficacy, improvement of function and reduction of side effects of drugs. Herein, Poly (ε-caprolactone) (PCL)/Poly (N-vinyl-2-pyrrolidone) (PVP) core-shell nanofibers loaded by multi-walled carbon nanotubes (MWCNTs) were produced. The surfaces of nanofibers were coated by polypyrrole (PPy) via vapor phase and chemical method. The chemical method was desirable according to SEM images and electrical conductivity of about 502.89 ± 45.25 S/m. Electrical stimulation was performed in the coated sample and the release of 5-fluorouracil (5FU) was investigated. Drug release of non-coated and coated samples without/with field application was investigated. The results exhibited the electric signal could be considered as a drug release control factor for coated samples with electrical field application.

Polyethyleneimine (PEI) as a Polymer-Based Co-Delivery System for Breast Cancer Therapy.

Cancer has become one of the leading causes of morbidity and mortality worldwide. This disease is classified broadly by tissue, organ, and system; different cancer types and subtypes require different treatments. Drug bioavailability, selectivity, and high dosage, as well as extended treatment, are significantly associated with the development of resistance – a complex problem in cancer therapy. It is expected that the combination of anticancer drugs and drug delivery systems, using polymers to increase the access of such agents to their site of action, will improve the efficacy of therapy. Polyethyleneimine (PEI) is a polymer used as a co-delivery system for anticancer drugs and gene therapy. PEI is also useful for other purposes, such as transfection and bio-adsorbent agents. In co-delivery, PEI can promote drug internalization. However, PEI with a high molecular weight is linked to higher cytotoxicity, thus requiring further evaluation of clinical safety. This review focuses on the utilization of PEI as a co-delivery system for anticancer therapy, as well as its potential to overcome resistance, particularly in the treatment of specific subtypes (eg, breast cancer). In conclusion, PEI has promising applications and is improvable for the development of anticancer drugs.

Interface‐cross‐linked micelles of poly(D,L‐lactide)‐b‐poly(furfuryl methacrylate)‐b‐poly(N‐acryloylmorpholine) for near‐infrared‐triggered drug delivery application

AbstractIn this study, we report a near‐infrared (NIR)‐responsive interface cross‐linked (ICL) micelles prepared by using the Diels–alder (DA) click reaction between poly(D,L‐lactide)‐b‐poly(furfuryl methacrylate)‐b‐poly(N‐acryloylmorpholine) (PLA‐b‐PFMA‐b‐PNAM) triblock copolymers and a diselenide cross‐linker, bis(maleimidoethyl) 3,3′‐diselanediyldipropionoate (BMEDSeDP). PLA‐b‐PFMA‐b‐PNAM was synthesized by the sequential RAFT polymerization of FMA and NAM using PLA‐macro‐chain transfer agent (PLA‐CTA) as a macro‐initiator. The DA reaction between BMEDSeDP and the furfuryl moiety in the triblock copolymer resulted in the formation of ICL micelles. The ICL micelles were analyzed by 1H NMR, FE‐SEM and DLS methods. An anticancer drug, doxorubicin (DOX) was in situ incorporated into the ICL micellar core to prepare drug loaded ICL micelles. The release of DOX from the ICL micelles was suppressed (ca. 11% in 60 h) under physiological conditions (pH 7.4), indicating that the interfacial cross‐linking greatly protected the drug release from the micelles. Interestingly, the DOX‐loaded ICL micelles showed pH and NIR‐responsive drug release profile, and the highest release was observed under NIR laser irradiation at pH 5.0. The in vitro toxicity analysis demonstrated that the ICL was not basically cytotoxic against normal HFF‐1 cells (non‐cancerous), while higher antitumor activity towards HeLa cells were exhibited by DOX‐loaded ICL micelles. The developed ICL micelles would provide a promising robust anticancer drug delivery system for the future cancer treatment.

Polysaccharide-Drug Conjugates: A Tool for Enhanced Cancer Therapy.

Cancer is one of the most widespread deadly diseases, following cardiovascular disease, worldwide. Chemotherapy is widely used in combination with surgery, hormone and radiation therapy to treat various cancers. However, chemotherapeutic drugs can cause severe side effects due to non-specific targeting, poor bioavailability, low therapeutic indices, and high dose requirements. Several drug carriers successfully overcome these issues and deliver drugs to the desired sites, reducing the side effects. Among various drug delivery systems, polysaccharide-based carriers that target only the cancer cells have been developed to overcome the toxicity of chemotherapeutics. Polysaccharides are non-toxic, biodegradable, hydrophilic biopolymers that can be easily modified chemically to improve the bioavailability and stability for delivering therapeutics into cancer tissues. Different polysaccharides, such as chitosan, alginates, cyclodextrin, pullulan, hyaluronic acid, dextran, guar gum, pectin, and cellulose, have been used in anti-cancer drug delivery systems. This review highlights the recent progress made in polysaccharides-based drug carriers in anti-cancer therapy.

Impact of ErbB Receptors and Anticancer Drugs against Breast Cancer: A Review.

Human EGFR (epidermal growth factor receptor) family of tyrosine kinase receptors consists of four members, ErbB1-4. Abnormalities in the ErbB family characterize a variety of human cancers, including breast cancer. Tyrosine kinase is recruited by the activated EGFR cell surface receptor, which transmitted signals from the receptor to interact with intracellular signaling pathways and regulate cellular functions and biological processes. Targeting the intracellular signaling pathways has been aided in the drug development that was already in use and more continually being developed. The review article highlights the function of ErbB receptors/ligands, their role in signaling pathways, effective targeted drugs, and a combination of targeted drug strategies in the treatment of breast cancer that could be leading to the novel combination of anticancer drug delivery systems.

Folic Acid-Adorned Curcumin-Loaded Iron Oxide Nanoparticles for Cervical Cancer.

Cancer is a deadly disease that has long plagued humans and has become more prevalent in recent years. The common treatment modalities for this disease have always faced many problems and complications, and this has led to the discovery of strategies for cancer diagnosis and treatment. The use of magnetic nanoparticles in the past two decades has had a significant impact on this. One of the objectives of the present study is to introduce the special properties of these nanoparticles and how they are structured to load and transport drugs to tumors. In this study, iron oxide (Fe3O4) nanoparticles with 6 nm sizes were coated with hyperbranched polyglycerol (HPG) and folic acid (FA). The functionalized nanoparticles (10–20 nm) were less likely to aggregate compared to non-functionalized nanoparticles. HPG@Fe3O4 and FA@HPG@Fe3O4 nanoparticles were compared in drug loading procedures with curcumin. HPG@Fe3O4 and FA@HPG@Fe3O4 nanoparticles’ maximal drug-loading capacities were determined to be 82 and 88%, respectively. HeLa cells and mouse L929 fibroblasts treated with nanoparticles took up more FA@HPG@Fe3O4 nanoparticles than HPG@Fe3O4 nanoparticles. The FA@HPG@Fe3O4 nanoparticles produced in the current investigation have potential as anticancer drug delivery systems. For the purpose of diagnosis, incubation of HeLa cells with nanoparticles decreased MRI signal enhancement’s percentage and the largest alteration was observed after incubation with FA@HPG@Fe3O4 nanoparticles.

Guar gum-g-poly(N-acryloyl-L-phenyl alanine) based pH responsive smart hydrogels for in-vitro anticancer drug delivery

ABSTRACT In this study, modified natural polymeric-based pH-responsive hydrogels (GNAHs) were formulated using guar gum-grafted-poly(N-acryloyl phenyl alanine), 2-hydroxy ethyl acrylate, and 2-acrylamido-2-methyl-1-propane sulfonic acid. GNAH hydrogels were synthesized using a single-step radical polymerization reaction using N,N’-methylenebisacrylamide as a crosslinker and potassium persulfate as an initiator. The GNAH was used for the controlled release of Imatinib mesylate (IMS), an anticancer drug. The FTIR spectroscopy confirmed the IMS loading as well as grafting reaction between GG-g-PNPA and PHEA-co-PAMPS. This was further confirmed by XRD and DSC studies. The IMS also reduced the negative surface charge of the GNAH hydrogel. The microscopic images showed that the GNAH hydrogels have porous and canal structures with IMS molecules entrapped within the pores. The mode of drug release mechanism was assessed by applying various kinetic equations (non-Fickian diffusion mechanism, Higuchi square root and Korsmeyer–Peppas kinetic models) that showed pH-dependent drug release of hydrogels exhibiting an excellent controlled-release pattern for IMS for more than 48 h. Based on the drug release behavior of the as-synthesized amino acid-functionalized hydrogel, it can be suggested that GNAH hydrogels could also be used as a potential pH-responsive anticancer drug delivery system for other anticancer drugs.

Formulation and Characterisation of RGD-FBG Based Nanoscaffolds as Novel Anti-Cancer Drug Delivery System

Aims/Objective: To formulate and evaluate RGD sequenced fibrin/fibrinogen based nanoscaffolds (acid-labile linker) for the treatment of brain tumor targeting to achieve an acid-triggered drug release under a mild acidic condition in tumor.
 Place and Duration of Study: Department of Pharmaceutics, Parul Institute of Pharmacy and Research, Parul University, Vadodara, between 2017 to 2021.
 Methodology: Nanoscaffolds was prepared with Drug–linker–Fbg conjugate solution, using modified water-in-oil (W/O) emulsification/solvent extraction method. The conjugate solution was constantly injected in soya lecithin (100 ml) using a syringe (1 ml/min) and stirred using Magnetic stirrer for 30 minutes to form stable a W/O emulsion. The present investigation was aimed to evaluate with Particle size, Zeta potential measurement, Percent drug entrapment, Transmission electron microscopy.
 Results: As per Evaluation parameters were performed such as Particle size measured as 151.8±2.02 nm to 157.4 ± 3.81 nm. Zeta Potential was found that -37.1±6.32, Percent Drug Entrapment was 91.4±0.37 which indicates that the drug release of lyophilised FBG based nanoscaffolds was indicatively higher as compared to FBG based nanoscaffolds (alone).
 Conclusion: As per the study design the formulated nanoscaffolds were found to impart the drug release based on their particle size and percent drug entrapment and hence fights against cancer cells in brain by their EDC-NHS chemistry. Drug of choice Everolimus along with Fbg based nanoscaffolds offers better biocompatibility by exposing dual responsiveness at acidic environment in tumors. The results of in-vitro drug release reveals the better uptake of drug at targeted site of action.

Synthesis and controlled drug release behavior of micro-mesoporous wollastonite nanoparticles. Effect of calcination temperature on the structural and biodegradability properties

In this study, amorphous and crystalline (Pseudowollastonite) phases of wollastonite (CaSiO3) nanoparticles were successfully synthesized by a facile soft-template method with a micro-mesoporous structure. In addition, the effect of calcination temperature on the structural properties, surface charge, and biodegradability of synthesized nanoparticles were investigated. After that, the drug loading capacity and drug release behavior of the sample calcined at the lowest calcination temperature (600 °C, MMW-600) was investigated with Epirubicin (EPI) as an anti-cancer drug. Noticeably, MMW-600 showed the most appropriate (bio) properties as a candidate of drug carrier in comparison with the samples that calcined at higher temperatures by showing: the least hydrodynamic size (85 nm), the highest specific surface area (301.68 m2g) as well as micro-and mesopore volumes as 0.075 and 0.282 cm3g, respectively. Moreover, it indicated the lowest thickness of the pore wall (6.73 nm) and the highest rate of biodegradation in Tris-HCl. The investigation of drug release behavior revealed a pH-controlled release due to the pH-dependent surface charge of micro-mesoporous wollastonite (MMW) nanoparticles, which was demonstrated by Zeta potential analysis. Additionally, MMW nanoparticles demonstrated a desired high rate and sustained release of EPI (44% and 80% after 4 and 70 h, respectively) in succinate buffer (pH 5.5, mimic the pH of a tumor site). In conclusion, MMW can be a great candidate as a pH-controlled release drug-nanocarrier for anti-cancer drug delivery systems.

Dual responsive tamarind gum-co-poly(N-isopropyl acrylamide-co-ethylene glycol vinyl ether) hydrogel: A promising device for colon specific anti-cancer drug delivery

In this study, pH and temperature-sensitive tamarind gum (TM)-based hydrogels were synthesized by free radical polymerization using a combination of acrylamide (AM), N-isopropyl acrylamide (NIPAM), and ethylene glycol vinyl ether (EGVE) monomers with bis (2-(methacryloyloxy) ethyl phosphate (BMEP) as a crosslinker (TANEB hydrogel). The prepared TANEB hydrogels were characterized by Fourier transform infrared spectroscopy, X-ray diffraction (XRD), and scanning electron microscopy to confirm the formation of functional group interactions and morphology. 5-Fluorouracil (5-FU) as a model drug was loaded into the TANEB hydrogels. Differential thermal calorimetry and XRD confirmed the molecularly loaded 5-FU into TANEB hydrogels. Swelling studies revealed the dual responsive nature of the TANEB hydrogels. An in vitro drug release study was performed at pH 1.2 and 7.4 and at 25 and 37 °C. The release time of 5-FU from the hydrogels was extended up to 12 h. Also, 5FU encapsulated hydrogels showed remarkable cytotoxicity against human colorectal adenocarcinoma cancer cells (HCT116 cells) along with good cell cycle ability. Thus, the TANEB hydrogel formulations could be used as potential delivery system for anticancer drugs.

Magnetic ZnO/CdO Nanocomposite for Effective Drug Delivery System for Cancer Therapy

ZnO, ZnO/CdO, and Magnetic Ni-ZnO/CdO nanocomposite have been eco-friendly synthesized using Black Rice Husk Extract (BRHE) and water instead of hazardous chemicals and solvents. The anticancer drug Doxorubicin (Dox) was loaded on the PVA-coated biomimetic nanomaterials. The successful synthesis of the pure nanomaterials and the Dox-nanomaterial systems has been confirmed by evaluating their structural, crystalline, textural, surface, and optical properties using various characterization techniques. The Dox-nanomaterials systems were used as anticancer drugs against HEPG2 cells as a model of human cancerous cells. The in vitro Dox release was slower and more sustained from Ni-ZnO/CdO composite compared to the other individual nanomaterials, suggesting that a hydrogen bond strongly attached more Dox molecules to the surface Ni-ZnO/CdO. Moreover, the cytotoxicity investigations on the HEPG2 cell line showed that higher toxicity was obtained by Ni-doped nanocomposite, consistent with the results of in vitro release. This study provides novel magnetic Nanocarriers that can be used as anticancer drug delivery systems after more in vivo investigations on animals or clinical investigations.

Bioinspired quantum dots for cancer therapy: A mini-review

The global burden of cancer increases with the passing year and is becoming the primary cause of death globally. Chemotherapy plays an important role but produces side effects, natural compounds seem to be an option with fewer side effects, but their bioavailability remains a concern. Bioinspired Quantum dots (QDs) from plant sources show promising drug delivery and anti-cancer potential with low toxicity. QDs are well known for their optical activity and find their use in various applications and can be used explicitly for bio-imaging and drug delivery in cancer therapy. Further, bioinspired QDs as an anti-cancer drug delivery system is less explored. Thus, this featured article aims to conclude the recent advances in the use of bioinspired QDs for drug delivery in cancer therapy.

Fabrication of cellulose nanocrystals as potential anticancer drug delivery systems for colorectal cancer treatment

Polysaccharide nanocrystals have great potential to be used as improved drug carriers due to their low cost, high biodegradability, and biocompatibility. This study reports the synthesis of cellulose nanocrystals (CNC) loaded with 5-fluorouracil (CNC/5FU) to evaluate their anticancer activity against colorectal cancer cells. X-ray and Fourier-transform infrared spectroscopy demonstrated that acid hydrolysis successfully degraded the amorphous cellulose to liberate the crystal regions. From transmission electron microscopy, CNC/5FU appeared as rod-like nanocrystals with an average length and width of 69.53 ± 1.14 nm and 8.13 ± 0.72 nm, respectively. The anticancer drug 5FU showed improved thermal stability after being loading onto CNC. From UV–vis spectroscopy data, the drug encapsulation efficiency in CNC/5FU was estimated to be 83.50 ± 1.52%. The drug release of CNC/5FU was higher at pH 7.4 compared to those at pH 4.2 and 1.2. From the cytotoxicity assays, CNC did not affect the viability of CCD112 colon normal cells. On the other hand, CNC/5FU exhibited anticancer effects against HCT116 and HT-29 colorectal cancer cells. The anticancer actions of CNC/5FU against HCT116 cells were then confirmed using an in vitro tumor-on-chip model and clonogenic assay. Mechanistic studies demonstrated that CNC/5FU killed the cancer cells by mainly inducing cell apoptosis and mitochondrial membrane damage. Overall, this study indicated that CNC/5FU could be a potential nanoformulation for improved drug delivery and colorectal cancer treatment.

Highly-fluorescent BODIPY-functionalised metallacages as drug delivery systems: synthesis, characterisation and cellular accumulation studies.

With the aim of designing new metallosupramolecular architectures for drug delivery, research has focused on porous 3-dimensional (3D)-metallacages able to encapsulate cytotoxic agents protecting them from metabolism while targeting them to cancer sites. Here, two self-assembled [Pd2L4]4+ cages (CG1 and CG2) featuring 3,5-bis(3-ethynylpyridine)phenyl ligands (L) exo-functionalised with dipyrromethene (BODIPY) groups have been synthesised and characterised by different methods, including NMR spectroscopy and mass spectrometry. 1H NMR spectroscopy studies shows that the cages are able to encapsulate the anticancer drug cisplatin in their hydrophobic cavity, as evidenced by electrostatic potential (ESP) analysis based on XRD studies. The stability of the cages in an aqueous environment, and in the presence of the intracellular reducing agent glutathione, has been confirmed by UV-visible absorption spectroscopy. The luminescence properties of the cages enabled the investigation of their cellular uptake and intracellular localisation in human cancer cells by confocal laser scanning microscopy. In melanoma A375 cells, cage CG1 is taken up via active transport and endocytic trafficking studies show little evidence of transport through the early endosome while the cages accumulated in melanosomes rather than lysosomes. The antiproliferative activity of the lead cage was investigated in A375 together with two breast cancer cell lines, SK-BR-3 and MCF7. While the cage per se is non-cytotoxic, very different antiproliferative effects with respect to free cisplatin were evidenced for the [(cisplatin)2⊂CG1·BF4] complex in the various cell lines, which correlate with its different intracellular localisation profiles. The obtained preliminary results provide a new hypothesis on how the subcellular localisation of the cage affects the cisplatin intracellular release.