Phospholipid Nanoparticles Research Articles

The effect of lipid derivative of anti-tumor drug sarcolysin embedded in phospholipid nanoparticles in the experiments in vivo

To improve the therapeutic properties of the antitumor agent Sarcolysin, we have previously developed and characterized a dosage form representing its ester conjugate with decanol embedded in ultra-small phospholipid nanoparticles less than 30 nm in size ("Sarcolysin-NP"). The effect of the resulting composition was investigated in vivo in comparison with the free substance of sarcolysin. The composition intravenous administration to mice showed an improvement in the pharmacokinetic parameters of sarcolysin associated with its initial higher (by 22%) level in the blood and prolonged circulation, which was also observed in mice with P388 tumor. In mice with three types of tumors - lymphocytic leukemia P388, lymphocytic leukemia L1210, and adenocarcinoma of the mammary gland Ca755 - administration of two doses of sarcolysin over a period of 7 days showed its predominant antitumor effect. The maximum tumor growth inhibition was noted for lymphocytic leukemia L1210 and adenocarcinoma of the mouse mammary gland Ca755 (at a dose of Sarcolysin-NP - 8,4 mg/kg), which was higher in comparison with free substance by more than 24% and 17%, respectively. Differences in the life span of the treated animals were revealed significantly at a dose of 10 mg/kg and amounted to 25% and 17,4% for lymphocytic leukemia P388 and L1210, respectively, and 11% for adenocarcinoma Ca755. In an experiment on rats, acute toxicity of Sarcolysin-NP administered intravenously showed that an average LD50 value 2-3 times exceeded a similar parameter for commercial preparations of free sarcolysin (Melphalan and Alkeran), which indicates its lower toxicity.

Chlorin e6 embedded in phospholipid nanoparticles equipped with specific peptides: Interaction with tumor cells with different aminopeptidase N expression

A promising direction in Biopharmaceuticals is the development of specific peptide-based systems to improve drug delivery. This approach may increase tumor specificity and drug penetration into the target cell. Similar systems have been designed for several antitumor drugs. However, for photodynamic therapy drugs, such studies are not yet enough. Previously, we have developed a method of inclusion of chlorin e6 (Ce6), a photosensitizer used in photodynamic therapy, in phospholipid nanoparticles with a diameter of up to 30 nm, and reported an increase in its effectiveness in the experiments in vivo. In this work, we propose to modify a previously developed delivery system for Ce6 by the addition of cell-penetrating (R7) and/or targeting NGR peptides. The interaction of the compositions developed with HepG2 and MCF-7 tumor cells is shown. The expression of CD13 protein with affinity to NGR on the surface of these cells has been studied using flow cytometry. The expression of this protein on the HepG2 cells and its absence on MCF-7 was demonstrated. After incubation of tumor cells with the resulting Ce6 compositions, we evaluated the cellular accumulation, photoinduced, and dark cytotoxicity of the drugs. After irradiation, the highest level of cytotoxicity was observed when R7 peptide was added to the system, either alone or in combination with NGR. In addition to R7, the NGR-motif peptide increased the internalization of Ce6 in HepG2 cells without affecting its photodynamic activity. In this work we also discuss possible mechanisms of action of the cell-penetrating peptide when attached to phospholipid nanoparticles.

Usage of a new pharmacological agent of ultra-small phospholipid nanoparticles (micelles) in the treatment of combined hyperlipidemia

Abstract Background and aims Based on the developed technology of prerparation of ultra small size phospholipid nanoparticles without the use of detergents/surfactants and stabilizers drug preparation, exhibiting hypolipidemic properties has been obtained. Preclinical studies have shown that phospholipid nanoparticles of 20–30 nm (PLN) activate reverse cholesterol transport. PLN is now at the stage of clinical trials (Phase II study completed). The aim of the study was to compare the efficacy, safety and tolerability of PLN relative to placebo in the treatment of combined hyperlipidemia. Methods This Phase III, multicenter, randomized, double-blind, placebo-controlled, parallel-group study was conducted at 4 centers. The patients (pts) received PLN or placebo (1:1), powder for oral solution preparation (in an aqueous environment is a nanoemulsion with a particle size of 20–30 nm), 500 mg (sachet) orally 2 times a day for 12 weeks. Lipid parameters, safety and tolerability were measured. The data is presented in M (s), Me (lq; hq). Mann-Whitney U Test was to compare the significant difference of groups. P value <0.05 was considered statistically significant. Results A total of 100 pts with combined hyperlipidemia were randomized (age 35–70 years, males 58%).The mean age of patients was 56.4 (10.2) years. Mean total cholesterol, non-high-density lipoprotein cholesterol (non-HDL-C), TG, and apolipoprotein B 100 (apoB) levels at baseline were 5.59 (0.8) mmol/l, 4.51 (0.75) mmol/l, 2.38 (0.6) mmol/l and 114.26 (24.96) mg/dl, respectively (n=100). Mean high-density lipoprotein cholesterol (HDL-C) and Lp(a) levels at baseline were 1.0 (0.25) mmol/l and 21.1 (3.9; 20.3)mg/dl, respectively (n=100). At Week 12, PLT significantly reduced total cholesterol, non-HDL-C levels, TG and apo B compared to placebo (p=0.02, p=0.03, p=0.001 and p=0.02, respectively). At the same time, the mean HDL-C level was significantly increased (p=0.03). The drug was well tolerated and no clinically significant laboratory abnormalities were detected. Conclusions This study demonstrates that therapy with PLT is well tolerated in additional beneficial effects on key lipid parameters in patients with moderate combined hyperlipidemia. Funding Acknowledgement Type of funding source: Public Institution(s). Main funding source(s): Ministry of industry and trade

Chlorine e6 in Phospholipid Nanoparticles with Specific Targeting and Penetrating Peptides as Prospective Composition for Photodynamic Therapy of Malignant Neoplasms

Chlorine e6 in Phospholipid Nanoparticles with Specific Targeting and Penetrating Peptides as Prospective Composition for Photodynamic Therapy of Malignant Neoplasms

Development, characterization and solubility enhancement of BCS class II drug phenytoin by solid phospholipid dispersion technique

The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. Phenytoin is taking as a model drug; the present study adopted an innovative solid phospholipid nanoparticle (SPLN) line of attack, and it is parallelly equated with the industrialized methods (freeze-drying) which are used for the boosting of solubility and dissolution of Phenytoin. Phenytoin was articulated along with phospholipid and mannitol at a diverse ratio of phenytoin, PL, mannitol, in which 1:12:18 was the correct ratio for ideal preparation. Freeze-drying helps to prepare SPLNs in orbicular shape, which is amorphous in nature with ≤ 1µm diameter on average. While the amorphous matrix-like structure of solid phospholipid dispersion with larger particle size is obtained by freeze-drying technique. Formulating the formulation from this method improved the dissolution rate in a remarkable way. Tris buffer with pH 7.4acts as an apparent solubility dissolved concentration of phenytoin. The poor aqueous solubility acts as a core challenge in oral dosage form development for BCS class II drugs. The decrease in the particle size or cumulating the drug surface area is the widely used practices to proliferate the solubility. The target of the present work was improvisation in solubility, dissolution of a poorly water-soluble drug, and its release by using solid phospholipid nanoparticles. Phenytoin is taking as a model drug. The solid phospholipid nanoparticles were primed by freeze-drying technique along with phospholipid and mannitol in diverse drug to excipients ratios (1:1, 1:2w: w). These preparations were assessed for compatibility study using FTIR, solubility enhancement study by XRD, entrapment efficiency, surface morphology by SEM, and in-vitro release study. As per the results, there is no influence of the excipients on the drug used. The solubility was increased by folds compared to in house prepared formulation.

Targeted drug delivery system for doxorubicin based on a specific peptide and phospholipid nanoparticles

Doxorubicin is one of the widely known and frequently used chemotherapy drugs for the treatment of various types of cancer, the use of which is difficult due to its high cardiotoxicity. Targeted drug delivery systems are being developed to reduce side effects. One of the promising components as vector molecules (ligands) are NGR-containing peptides that are affinity for the CD13 receptor, which is expressed on the surface of many tumor cells and tumor blood vessels. Previously, a method was developed for preparing a composition of doxorubicin embedded in phospholipid nanoparticles with a targeted fragment in the form of an ultrafine emulsion. The resulting composition was characterized by a small particle size (less than 40 nm) and a high degree of incorporation of doxorubicin (about 93%) into transport nanoparticles. When assessing the penetrating ability and the degree of binding to the surface of fibrosarcoma cells (HT-1080), it was shown that when the composition with the targeted fragment was added to the cells, the level of doxorubicin was almost 2 times higher than that of the liposomal form of doxorubicin, i.e. the drug in the system with the targeted peptide penetrated the cell better. At the same time, on the control line of breast adenocarcinoma cells (MCF-7), which do not express the CD13 receptor on the surface, there was not significant difference in the level of doxorubicin in the cells. The data obtained allow us to draw preliminary conclusions about the prospects of targeted delivery of doxorubicin to tumor cells when using a peptide conjugate containing an NGR motif and the further need for its comprehensive study.

Effect of Cell-Penetrating Arginine Peptide on Interaction of Photosensitizer Chlorin e6 Incorporated into Phospholipid Nanoparticles with Tumor Cells.

We studied the possibility of increasing the efficiency of photodynamic therapy by improving delivery of photosensitizers chlorin e6 into tumor cells. Previous studies showed that incorporation of chlorin e6 onto phospholipid nanoparticles with a diameter <20 nm reduces its cytotoxicity due to accelerated elimination from organs [8]. A heptapeptide R7 synthesized and added to this combination promoted internalization of chlorin e6 into HepG2 cells in comparison with initial nanoparticles without peptide R7. The observed effect of peptide R7 can be explained by activation of endocytosis and/or macropinocytosis (bearing in mind the interaction of arginine with carboxyl groups of e6. The development of this transporting system is a promising trend in photodynamic therapy of cancer diseases.

The Increase of Anti-tuberculosis Efficacy of Rifampicin Incorporated Into Phospholipid Nanoparticles with Sodium Oleate

The Increase of Anti-tuberculosis Efficacy of Rifampicin Incorporated Into Phospholipid Nanoparticles with Sodium Oleate

Phospholipid nanoformulation of thymoquinone with enhanced bioavailability: Development, characterization and anti-inflammatory activity

Thymoquinone (TQ), a potent bioactive of Nigella sativa plant, is highly hydrophobic molecule and thus associated with poor oral bioavailability. The present work proposes the phospholipid-nanoparticles (PLN) based delivery of TQ to enhance the low oral bioavailability and anti-inflammatory activity. TQ-loaded nanoparticles were prepared via micro-emulsification technique employing different phospholipid concentrations and extensively characterized for particle size, surface charge, surface morphology, entrapment efficiency, and drug release kinetics. Further, the nanoparticles were assessed for oral bioavailability, and anti-inflammatory activity employing rat paw edema model. The optimized nanoparticle composition (F1) was nanosized (<100 nm) with spherical morphology coupled with narrow size distribution, higher drug entrapment efficiency (>70%), controlled drug release pattern, and negatively charged surface (zeta potential of −0.57 mV). After oral administration of a single dose of F1 formulation, showed approx. 226.6% relative bioavailability vis-à-vis plain TQ suspension. While, substantially higher reduction in the percent inhibition in paw edema in comparison to the pure drug suspension and diclofenac sodium, was observed in the inflammation model. The present work indicate that PLN could be an efficient nanodevices for the treatment of inflammatory disorders and promising carrier system to augment TQ oral bioavailability.

Antibiotic-Derived Lipid Nanoparticles to Treat Intracellular Staphylococcus aureus.

Intracellular survival of pathogenic bacteria leads to high chances of bacterial persistence and relapse in the bacteria-infected host. However, many antibiotics fail to clear the intracellular bacteria due to their low internalization by cells. In order to increase delivery of antibiotics in cells and eliminate intracellular bacteria, we developed antibiotic-derived lipid nanoparticles. First, we synthesized antibiotic-derived lipid conjugates using two widely used antibiotics including penicillin G (PenG) and levofloxacin (Levo). Then, we formulated them into antibiotic-derived lipid nanoparticles and evaluated their antibacterial effects. We found that penicillin G derived phospholipid nanoparticles (PenG-PL NPs) were able to enhance cellular uptake of penicillin G as compared with free penicillin G and eliminate up to 99.9998% of ~108.5 intracellular methicillin sensitive Staphylococcus aureus (S. aureus) in infected A549 cells, a lung epithelial cell line. The PenG-PL NPs showed the potential for inhibiting intracellular S. aureus and are promising to be further studied for in vivo antibacterial applications.

Nanoparticle Based Treatment for Cardiovascular Diseases.

Nanotechnology has gained increased attention for delivering therapeutic agents effectively to the cardiovascular system. Heart targeted nanocarrier based drug delivery is a new, effective and efficacious approach for treating various cardiac related disorders such as atherosclerosis, hypertension, and myocardial infarction. Nanocarrier based drug delivery system circumvents the problems associated with conventional drug delivery systems, including their nonspecificity, severe side effects and damage to the normal cells. Modification of physicochemical properties of nanocarriers such as size, shape and surface modifications can immensely alter its invivo pharmacokinetic and pharmacodynamic data and will provide better treatment strategy. Several nanocarriers such as lipid, phospholipid nanoparticles have been developed for delivering drugs to the target sites within the heart. This review summarizes and increases the understanding of the advanced nanosized drug delivery systems for treating cardiovascular disorders with the promising use of nanotechnology.

Induction of lipid droplets in non-macrophage cells as well as macrophages by liposomes and exosomes

It has been reported that phospholipid nanoparticles (PNPs) including liposomes and exosomes could efficiently induce lipid droplets (LDs) in macrophages. However, in non-macrophage cells, the effects of PNPs on the induction of LDs have not been thoroughly investigated. In this report, we directly compared non-macrophage and macrophage cell lines in terms of LD induction by various formulation of liposomes containing phosphatidylserine and exosomes. All non-macrophage cell lines as well as macrophage cell lines tested in this study showed evident LD induction in response to these PNPs, though the efficacy of LD induction in non-macrophage cell lines varied considerably. Our results suggest that LD formation is a common and crucial response to PNPs in mammalian cells not only in macrophages but also in non-macrophage cells.

Chlorine e6 in phospholipid nanoparticles with specific targeting and penetrating peptides as prospective composition for photodynamic therapy of malignant neoplasms

Cytotoxic and photoinduced activity of chlorine e6 (Ce6) in phospholipid nanoparticles with specific tumor targeting and cell-penetrating peptides was studied in vitro using human fibrosarcoma cells HT-1080. It was shown, that the binding of cell-penetrating peptide R7 - alone or combined with the peptide containing specific targeting motif NGR (Asn-Gly-Arg) - resulted in 3-fold decrease of Ce6 photoinduced activity as compared with that in nanoparticles without peptides (IC50 values were 0.7 μg/ml and 2.1 μg/ml, respectively). The NGR influence was unexpectedly low - less than 20% (IC50 1.7 μg/ml). This suggests the more importance of Ce6 cell penetration in this case, than of NGR-mediated targeting. The effect of inclusion of both peptides on the total cytotoxicity of Ce6 was minimal (10-16 times less than on the specific photoinduced activity). The obtained results - together with earlier shown effects on improvement of the pharmacokinetics of Ce6 in vivo after its embedding into phospholipid nanoparticles - indicate the prospects of using the obtained phospholipid nanoparticles system for photodynamic therapy.

Prednisolone in phospholipid nanoparticles: prolonged circulation and increased antiinflammatory effect

Along with modern new drugs, many therapeutic schemes also include known effective drugs, particularly, glucocorticoids. One of the most distributed of them is prednisolone that has pronounced anti-inflammatory properties. Its disadvantage is short-term circulation, resulting in a number of side effects. For this reason the development of its more effective and safe formulations is carried out. We have obtained the formulation of prednisolone included in nanoparticles from soy phosphatidylcholine with an average diameter of 20 nm. With oral administration to rats and analysis by HPLC an increase in prednisolone maximal concentration in of plasma and the duration of circulation as compared with free drug administration were shown. The experiment with mice with conconavalin A induced inflammation was also carried out: conconavalin A was injected subplantary in an hour after oral administration of both prednisolone formulations in several doses. The index of the inflammatory reaction (determined by the edema degree) was suppressed more effectively in the case of prednisolone in nanoparticles. Maximal suppression (62.2% as compared with 49.6% for free prednisolone) was observed even at a minimal dose (2.5 mg/kg), at which the free drug did not act at all. The results indicate an increase in the efficiency of prednisolone included in phospholipid nanoparticles, that makes it possible to diminish its administered doses and thereby reduce the risk of side effects.

Preparation and Properties of Antitumor Drug Based on Lipid Derivative of Sarcolysin

The conditions for the preparation of a drug formulations based on the lipid derivative of sarcolysin embedded in phospholipid nanoparticles have been optimized. The drug is an ultra-thin emulsion with a light transmittance above 80% and a particle size of not more than 50 nm. It should be noted that 99% of the lipid derivative of sarcolysin are incorporated into phospholipid nanoparticles. Preservation of aggregation stability in the aquatic environment was observed for at least 2 days. In vitro experiments have shown that sarcolysin, introduced as a part of phospholipid nanoparticles, is distributed among lipoproteins and protein components of plasma. Moreover, the content of sarcolysin in all fractions involved in the transport of biologically active substances in the body, is significantly higher in case of prodrug administration (lipid derivative of sarcolysin) in the composition of phospholipid nanoparticles than, as compared with administration of a free form (pharmacological substances) to the incubation medium. The transformation of a prodrug into the drug sarcolysin occurs in the blood cells.

Role of zein incorporation on hydrophobic drug-loading capacity and colloidal stability of phospholipid nanoparticles.

Liposome, phosphatidylcholine nanoparticle (PC-NP), is an attractive colloidal carrier of hydrophobic drugs but its clinical development is often limited by low drug-loading capacity and the physical instability. Zein is a water-insoluble amphiphilic protein obtained from the corn. We herein investigated a possibility to develop zein-phosphatidylcholine hybrid nanoparticle (Z/PC-NP) as an advanced hydrophobic drug carrier. By employing the conventional liposome preparation method with the addition of zein, Z/PC-NP were produced. The extent of zein incorporation in PC-NP was affected by PC composition. DSC demonstrated the lowered phase transition temperature of PC by zein and FTIR showed the appearance of weakened but clear amide bonds of zein as well as increased levels of heterogeneous hydrogen bonding of Z/PC-NP compared to PC-NP. DLS, TEM and cryo-TEM studies suggested Z/PC-NP to be spherical nanoparticles composed of a zein core and a zein-PC hybrid shell. Z/PC-NP exhibited a higher loading capacity for hydrophobic model drugs (paclitaxel, docetaxel, celecoxib and curcumin), than did the zein nanoparticle and PC-NP, while exhibiting an intermediate drug release rate. The serum stability and the storage stability of Z/PC-NP were greater than those of PC-NP. Zein functioned as a cryoprotectant of PC-NP during freeze-drying. Z/PC-NP may provide a promising nanoparticle carrier of hydrophobic drugs.

Development of phospholipid nanoparticles encapsulating 3-O-cetyl ascorbic acid and tocopherol acetate (TA-Cassome) for improving their skin accumulation

Phospholipid nanoparticles (PNs) encapsulating vitamin C and E derivatives, 3-O-cetyl ascorbic acid (CA) and tocopherol acetate (TA), respectively, were examined using the film rehydration and extrusion method. PN formulations (TA-Cassome) were prepared by mixing CA, soya phosphatidylcholine (Soya PC), sodium cholate, and TA at a molar ratio of 20/80/5/6. Glycerol (GL) or diglycerol (DG) were also added to improve the skin accumulation of CA and TA. Three TA-Cassome formulations were evaluated using a dynamic light scattering (DLS), NMR, TEM, skin accumulation test for CA and TA, and small-angle X-ray diffraction (SAXD) analysis. TA-Cassome formulations (150 nm) were stable for two weeks and they encapsulated 1.8 mg/mL of TA. TEM and SAXD analysis revealed that the nanoparticles formed a spherical multilayer structure. 1H and 31P NMR indicated that GL and DG enhanced the proton mobility of choline groups of soya PC molecules located on the membrane surface of TA-Cassome. Accumulation of CA and TA in the dermis was increased by adding GL and DG. SAXD analysis revealed that GL and DG promoted the formation of new lamellar structures on the stratum corneum, which contributed to improving the skin accumulation of CA and TA.

Targeted therapy of triple negative MDA-MB-468 breast cancer with curcumin delivered by epidermal growth factor-conjugated phospholipid nanoparticles.

Triple-negative breast cancer (TNBC) is associated with poor survival as chemotherapy is currently limited to conventional cytotoxic agents. Curcumin has promising anticancer actions against TNBC, but its application is hindered by poor bioavailability and rapid degradation in vivo. In the present study, curcumin-loaded phospholipid nanoparticles (Cur-NPs) conjugated with epidermal growth factor (EGF) were prepared for specific targeting of EGF receptors overexpressed in TNBC. NP formulation was performed by reacting EGF peptide with N-hydroxysuccinimide-Polyethylene Glycol-1,2-Distearoyl-sn-Glycero-3-Phosphoethanolamine (NHS-PEG10000-DSPE), followed by efficient curcumin loading through lipid film hydration. EGF conjugation did not significantly affect NP size, zeta potential or morphology. Specific targeting was confirmed by EGF receptor activation and blocking of 125I-labeled NP binding by excess EGF. EGF-Cur-NP dose-dependently suppressed MDA-MB-468 TNBC cell survival (IC50, 620 nM), and completely abolished their capacity to form colonies. The cytotoxic effects were more potent compared with those of free curcumin or Cur-NP. In mice bearing MDA-MB-468 tumors, injections of 10 mg/kg EGF-Cur-NP caused a 59.1% retardation of tumor growth at 3 weeks compared with empty NP, whereas the antitumor effect of Cur-NP was weak. These results indicate that EGF-conjugated NHS-PEG10000-DSPE phospholipid NPs loaded with curcumin may be useful for treating TNBCs that overexpress the EGF receptor.

The condition optimization and mechanism of aerobic phosphorus removal by marine bacterium Shewanella sp.

Excessive release of phosphorus (P) from wastewater into water systems is a significant environmental problem. Aerobic P removal, a new P removal pathway, was investigated. P removal primary mechanisms of marine bacteria Shewanella sp. CF8-6 (S. sp. CF8-6) were studied by batch tests and characterization analysis. The strain showed wide environmental adaptability (temperature 5.0–35.0 °C, dissolved oxygen (DO) 5.2–8.6 mg/L, pH 5.8–9.6, salinity 0.0–10.0%, P concentration 1.1–11.7 mg/L and COD/N (C/N) 7–13) and a relatively high P removal performance under strict aerobic conditions. The optimum conditions of P removal by S. sp. CF8-6 was: temperature 25.0 °C, DO 7.83 mg/L, pH 7.2, salinity 5.0%, P concentration 11.74 mg/L and C/N 13. The higher P removal rate was associated with better biomass growth of S. sp. CF8-6 in general, but the strategy of biomass-independent P removal was also indicated. Only a small percentage (20.0%) of removed P contributed by bacterial growth and intracellular metabolism, while a considerable part (up to 60%) was reserved in extracellular polymeric substances (EPS) in the form of extracellular phospholipid nanoparticles. The scanning electron microscope-energy dispersive spectrometer (SEM-EDS) results indicated the element in the accumulation nanoparticles was carbon, oxygen, sodium and P. The 31P nuclear magnetic resonance (NMR) analysis illustrated that orthophosphate monoester was the only intracellular P species, while both orthophosphate monoester and diesters existed extracellularly. Batch treatment of actual wastewater showed S. sp. CF8-6 had application potential in saline wastewater treatment. This study introduced a new pathway of P accumulation and removal. Application of marine bacteria S. sp. CF8-6 provided us an alternative method for P removal, especially in saline wastewater.

Comparison of a new nanoform of the photosensitizer chlorin e6, based on plant phospholipids, with its free form.

Photodynamic therapy is an advanced method of treating cancer and various benign diseases, including infections. It uses light‐activated molecules [photosensitizers (PSs)] to generate reactive oxygen species (ROS) when irradiated with light of a specific wavelength. This study examined the photophysical and photosensitizing activity of the PS chlorin e6 incorporated in a delivery system based on plant phospholipids. This new nanoform of chlorin e6 comprised particles with a diameter of 18.4 ± 2.5 nm and zeta potential of −34.6 ± 3.0 mV. Incorporation of chlorin e6 in phospholipid nanoparticles was observed to cause a bathochromic shift of Q‐band absorption maximum by 14 nm without an absorption change in the range of the Soret band. Fluorescence intensity of chlorin e6 embedded in the phospholipid nanoparticles increased 1.7‐fold. Chlorin e6 in phospholipid nanoparticles, when irradiated, was able to generate ROS as shown by oxidation of polyunsaturated fatty acids of the phospholipid matrix of the delivery system and reduced l‐glutathione. In vivo it was demonstrated that the new nanoform of chlorin e6 provides more accumulation of PSs in tumor tissue than its free form. Moreover, its accumulation in the skin was lower and its elimination from the skin almost five times faster than when administered in free form. The observed differences of this new nanoform of chlorin e6 should lead to enhancement of antitumor efficacy and a decrease in phototoxicity.