Liposomal Delivery System Research Articles

Calcium voltage-gated channel subunit alpha 1C and glial fibrillary acidic protein signaling pathways as a selective biomarker in predicting the efficacy of liposomal loaded co-enzyme Q in the autistic rat model.

Autism spectrum disorder (ASD) is an extreme neuropsychotic disturbance with both environmental and genetic origins. Sodium propionate (PPA) a metabolic bioproduct of gut microbiota is well-thought-out as a successful autism animal model. Nevertheless, Liposomal drug delivery system possess the advantagous of biocompatibility, targeting organs, ability to carry large drug payloads and skipping macrophages for this purpose the current study was carried out to investigate the hypothesis that Calcium Voltage-Gated channel subunit alpha 1C (CACNA1C) and glial fibrillary acidic protein (GFAP) signaling pathways crosstalk with the efficacy of Co-enzyme Q10 (Co-Q10) and liposomal loaded Co-enzyme Q10 (L Co-Q10) in PPA mediated autistic rat model. Autism was conducted by buffered PPA (500mg/Kg b.wt) daily for 5 consecutive days subsequently treatment via Co-Q10 in a dose of (10mg/kg b.wt) and L Co-Q10 (2mg/kg b.wt) for four weeks then the autistic model was followed for signs of autism at different time intervals of (one, two and four weeks). The control, PPA intoxicated, and treated groups were subjected to behavioral tests (Y-Maze and open field), antioxidant analysis, gene expression analysis, and histological examination at different time intervals of the study. The results revealed that Co-Q10 and L Co-Q10 significantly elevated antioxidative stress biomarkers, comprising superoxide dismutase (SOD), glutathione (GSH), and total antioxidant capacity (TAC). In addition, they significantly ameliorated the oxidative stress biomarker malondialdehyde (MDA). Meanwhile, they significantly downregulated GFAP and CACNA1C mRNA gene expressions, Co-Q10 and LCo-Q10 showed improvement in almost brain regions post PPA histopathological alterations, even better results were manifested via LCo-Q10 groups. These results showed the superiority of LCo-Q10 over Co-Q10 in competing autism. In conclusion: The administration of anti-inflammatory and antioxidant agents such as Co-Q10 and L Co-Q10 may represent a promising strategy to counteract pathological behaviors in ASD model via targeting organs, increasing retention time, and reducing side effects.

STING agonist delivery by lipid calcium phosphate nanoparticles enhances immune activation for neuroblastoma

Neuroblastoma (NB) is a common solid tumor in children and infants, the formation and regression of which is closely linked to the tumor-host immune relationship. Stimulator of interferon genes (STING) agonists, particularly cyclic dinucleotide (CDN), have promising potential in NB therapy by generating innate and adaptive immune stimulation, thus leading to tumor control. CDN delivery in vivo is challenging due to the negative charge, hydrophilicity, and susceptibility to degradation by phosphodiesterase, which hinders the effectiveness of CDN. Thus, our study proposed four methods to load CDN into liposomes, using 2′,3′-cGAMP as the model drug. Lipid nanoparticles were prepared, followed by physicochemical characterization. Subsequently, cellular inhibition and immune stimulation were investigated. As a result, lipid calcium phosphate nanoparticles (LCP-NPs) possessed the highest encapsulation efficiency among the four preparation methods, with a diameter of 82.57±3.72 nm. LCP-NPs maintained size stability under refrigeration conditions at 4°C within 48 h. The surface of the liposome was positively charged. Compared to free cGAMP, LCP-NPs resulted in a slower release, enhanced cytotoxicity against tumor cells, greater activation of the cGAS-STING pathway, and increased expression of the immune factors. Taken together, these findings clearly demonstrated the effectiveness of the liposomal delivery system for cGAMP and provided a promising strategy for the treatment of NB.

An X-ray activatable gold nanorod encapsulated liposome delivery system for mitochondria-targeted photodynamic therapy (PDT).

In this work, we developed a mitochondria-targeted nanomaterial for neoadjuvant X-ray-triggered photodynamic therapy of rectal cancer. Herein, we designed a biodegradable liposome incorporating a photosensitizer, verteporfin, to generate X-ray-induced reactive oxygen species, gold nanorods as radiation enhancers, and triphenylphosphonium as the mitochondrial targeting moiety. The average size of the nanocarrier was about 150 nm. Due to the synergetic effect between X-ray and a combination of verteporfin and gold nanorods, as well as precise site-targeted TPP-modified liposomal nanocarriers, our nanoconjugates generated sufficient cytotoxic singlet oxygen within the mitochondria under X-ray irradiation, triggering the loss of membrane potential and mitochondria-related apoptosis of cancer cells.

Current Advancements Related to Phytobioactive Compounds Based Liposomal Delivery for Neurodegenerative Diseases.

Neurodegenerative diseases are the most widely affected disease condition in an aging population. The treatment available reduces the elevated manifestations but is ineffective due to the drug's poor bioavailability, plasma stability, and permeability across the blood-brain barrier (BBB). Until now, no therapeutic compound has been able to stop the progression of neurodegenerative disease. Even the available therapeutic moiety manages it with possible adverse effects up to the later stage. Hence, phytobioactive compounds of plant origin offer effective treatment strategies against neurodegenerative diseases. The only difficulty of these phytobioactive compounds is permeability across the BBB. Engineered nanocarriers such as liposomes provide high lipid permeability across BBB. Liposomes have unique physicochemical properties that are widely investigated for their application in diagnosing and treating neurodegenerative diseases. The surface modification on liposomes by peptides, antibodies, and RNA aptamers offers receptor targeting. These brain-targeted approaches by liposomes improve the efficacy of phytoconstituents. Additional surface modification methods are utilized on liposomes, which increases the brain-targeted delivery of phytobioactive compounds. The marketing strategy of the liposomal delivery system is in its peak mode, where it has the potential to modify the existing therapy. This review will summarize the brain target liposomal delivery of phytobioactive compounds as a novel disease-modifying agent for treating neurodegenerative diseases.

Nonclinical Testing Evaluation of Liposomes as Drug Delivery Systems.

Various marketed drugs, as well as many in-development, have utilized liposomes, vesicles composed of one or more phospholipid bilayers, as a drug delivery system, often with the statement that they are "non-toxic" materials. This paper examined safety testing considerations and reviewed nonclinical packages used to support the safe clinical use and marketing of drugs using a liposomal drug delivery system, including liposome-only study findings. It was found that most experience has come from use of an established drug (especially in the oncology field) in a liposome formulation with known excipients. From this knowledge, it is proposed that the minimal package of studies (using an oncology indication as an example) needed to support clinical entry should include in vivo pharmacology in selected mouse xenograft models, pharmacokinetic characterization showing enhanced kinetics or disposition and including tumor exposure evaluation along with repeat-dose toxicity testing in one species. It was also found that the liposomes used in drug delivery systems are not truly "non-toxic" materials. However, the majority of findings in toxicity testing relate to macrophage processing of large amounts of lipid material, with no human known safety consequence. Of note, however, are cases of hypersensitivity for some PEGylated liposome forms which translate to the clinic.

Effects of Iron-Peptides Chelate Nanoliposomes on Iron Supplementation in Rats.

The objective of this study was to investigate the effects of iron nanoliposomes on iron supplementation and toxicity in SD rats induced by a low-iron diet. The size and infrared spectroscopy of a liposomal oral delivery system were investigated. The particle size of nanoliposomes embedded with chelates was increased. Infrared spectra proved that peptides-iron and blank nanoliposomes were bonded by interaction forces, including the fracture of hydrogen bonds, C = C bonds, hydrophobic interaction, and C-N bonds. We found that iron supplementation chelates had a certain protective effect on viscera after being embedded by nanoliposomes. After 10days of treatment, the concentration of hemoglobin could be gradually increased. Nanoliposome encapsulated peptides-iron has a better effect than other groups. At the same time, SOD, MDA, and CAT reached normal levels after 20days. Histological results showed that the sections of the nanoliposomes groups were clearer than those of the other groups. There was a little inflammation in the liver without obvious pathological changes, which also proved that the iron chelates embedded by nanoliposomes had no obvious side effects on iron supplementation in rats. Nanoliposome encapsulated peptides-iron has a small side effect and a significant curative effect of iron supplementation. It maybe has a good application prospect in the clinical medical field.

Cancer treatment: from traditional Chinese herbal medicine to the liposome delivery system

Traditional Chinese herbal (TCH) medicines have emerged as a prospective and affordable method to treat various diseases with a broad range of biological activity; however, traditional preparations, like decoctions, are often associated with low bioavailability, thus resulting in limited efficacy against cancer. The drawbacks of active TCH components, including instability, poor permeability, high hydrophilicity or hydrophobicity, undesirable pharmacokinetic profiles, and off-target toxicity, also exist. Most TCH medicines are thus limited to a clinical alternative for the treatment of chronic diseases. A liposomal delivery system is the most common class of FDA-approved nanomedicines, which has improved pharmacokinetics, enhanced targetability, and reduced side effects. Therefore, we anticipate that liposomal delivery technology will help concentrate drugs inside tumors, and fully release the therapeutic potential and reduce the side effects of TCH medicines. The review provides a brief overview of several representative TCH components and related liposome delivery strategies for enhanced cancer therapy. Current challenges associated with liposomal targeting of TCH medicines are also discussed for interested researchers.

Co-delivery of gemcitabine and salinomycin in PEGylated liposomes for enhanced anticancer efficacy against colorectal cancer

Colorectal cancer remains one of the major causes of morbidity and mortality in both developed and emerging countries. Cancer stem cells (CSCs) are a subpopulation of cells within the tumor mass harboring stem cell characteristics, considered responsible for tumor initiation, growth, relapse, and treatment failure. Lately, it has become clear that both CSCs and non-CSCs have to be eliminated for the successful eradication of cancer. Drug delivery systems have been extensively employed to enhance drug efficacy. In this study, salinomycin (SAL), a selective anti-CSC drug, and gemcitabine (GEM), a conventional anticancer drug, were co-loaded in liposomes and tested for optimal therapeutic efficacy. We employed the Design of Experiments approach to develop and optimize a liposomal delivery system for GEM and SAL. The antiproliferative effect of the liposomes was evaluated in SW-620 human colorectal cancer cells. The GEM and SAL-loaded liposomes exhibited adequate size, polydispersity, zeta potential, and drug content. The in vitro release study showed a sustained release of GEM and SAL from the liposomes over 72 h. Moreover, no sign of liposome aggregation was seen over 1 month and in a biological medium (FBS). The in vitro cytotoxic effects of the co-loaded liposomes were superior to that of single GEM either in free or liposomal form. The combination therapy using GEM and SAL co-loaded in liposomes could be a promising strategy for tackling colorectal cancer.

Formulation and Evaluation Tolbutamide Liposomes for a Sustained Drug Delivery System

Novel Drug Delivery system (NDDS) refers to the approaches, formulations, technologies, and systems for transporting a pharmaceutical compound in the body as needed to safely achieve its desired therapeutic effects. Applications of liposomes in medicine and pharmacology can be divided into diagnostic and therapeutic applications of liposomes containing various markers or drugs. The aim of the study was to formulate and evaluate Tolbutamide liposomes for a sustained drug delivery system. The tolbutamide was prepared as a liposomal drug delivery system by using two different techniques such as physical dispersion method and ether injection method. The morphological characters of prepared liposomes were determined with the help of optical microscope. The results of the particle size showed, when the concentration of soya lecithin was increased the size of the particle was reduced. The in vitro release showed that as the concentration of soya lecithin was increased the release rate of drug was retarded. Among the two methods ether injection method showed prolonged action when compared to physical dispersion method. The stability studies for all the formulations were performed by keeping the formulations at two different temperatures 4ºC±2ºC and 25ºC±2ºC for a period of 30 days. There was no change in morphological characters at 4ºC±2ºC, but there was a slight reduced in particles size at 25ºC±2ºC. The percentage drug entrapment was reduced in all the formulations at both the conditions.

Small-Angle Neutron Scattering Reveals the Nanostructure of Liposomes with Embedded OprF Porins of Pseudomonas aeruginosa.

The use of liposomes as drug delivery systems emerged in the last decades in view of their capacity and versatility to deliver a variety of therapeutic agents. By means of small-angle neutron scattering (SANS), we performed a detailed characterization of liposomes containing outer membrane protein F (OprF), the main porin of the Pseudomonas aeruginosa bacterium outer membrane. These OprF-liposomes are the basis of a novel vaccine against this antibiotic-resistant bacterium, which is one of the main hospital-acquired pathogens and causes each year a significant number of deaths. SANS data were analyzed by a specific model we created to quantify the crucial information about the structure of the liposome containing OprF, including the lipid bilayer structure, the amount of protein in the lipid bilayer, the average protein localization, and the effect of the protein incorporation on the lipid bilayer. Quantification of such structural information is important to enhance the design of liposomal delivery systems for therapeutic applications.

Liposomal amphotericin B-the past.

The discovery of amphotericin B, a polyene antifungal compound, in the 1950s, and the formulation of this compound in a liposomal drug delivery system, has resulted in decades of use in systemic fungal infections. The use of liposomal amphotericin B formulation is referenced in many international guidelines for the treatment of fungal infections such as Aspergillus and cryptococcal disease and Candida infections, as well as other less common infections such as visceral leishmaniasis. With the development of liposomal amphotericin B, an improved therapeutic index could be achieved that allowed the attainment of higher drug concentrations in both the plasma and tissue while simultaneously lowering the toxicity compared with amphotericin B deoxycholate. In over 30 years of experience with this drug, a vast amount of information has been collected on preclinical and clinical efficacy against a wide variety of pathogens, as well as evidence on its toxicity. This article explores the history and nature of the liposomal formulation, the key clinical studies that developed the pharmacokinetic, safety and efficacy profile of the liposomal formulation, and the available microbiological data.

Pheophorbide A-Mediated Photodynamic Therapy Potentiates Checkpoint Blockade Therapy of Tumor with Low PD-L1 Expression.

Although the immune checkpoint blockade (ICB) has made a great success in cancer immunotherapy, the overall response rate to the ICB, such as anti-programmed death ligand 1 (PD-L1) therapy, remains only at 20-30%. One major reason is the low expression level of the immune checkpoint in a certain type of tumor cells and its insufficient activation of the host immune system. Herein, we reported a cyclic RGD (cRGD)-modified liposomal delivery system loading the anti-PD-L1 antibody and the photosensitizer pheophorbide A (Pa), allowing a targeting of the low PD-L1 expressing 4T1 mouse breast cancer cells through the recognition of an overexpression of αvβ3 integrin on the tumor cells. The Pa-mediated photodynamic therapy (PDT) elevated the expression of PD-L1 on the tumor cells. PDT, in combination with the anti-PD-L1 therapy, promoted the activation and maturation of dendritic cells as well as the infiltration of cytotoxic T lymphocytes, resulting in the augmented antitumor immune response for the enhanced therapeutic effect. These results demonstrated the combined therapeutic effects of PDT and ICB on the tumor with low PD-L1 levels. Our study suggested that an increase in the PD-L1 expression in tumor cells by PDT would be a promising adjuvant treatment to overcome the ICB irresponsiveness.

Research progress on liposome and nanomicelle targeted drug delivery system across blood-brain barrier

The blood-brain barrier(BBB), a protective barrier between brain tissues and brain capillaries, can prevent drugs from entering the brain tissues to exert the effect, which greatly increases the difficulty in treating brain diseases. The drug delivery system across the BBB can allow efficient drug delivery across the BBB by virtue of carriers and formulations, thereby enhancing the therapeutic effect of drugs on brain tissue diseases. Liposomes and micelles have been extensively studied with advances in the targeted therapy across the BBB for the brain due to their unique structures and drug delivery advantages. This study summarized the research status of liposome and micelle drug delivery systems across the BBB based on the literature in recent years and analyzed their application advantages and mechanism in terms of trans-BBB capability, targeting, and safety. Moreover, the problems and possible countermeasures in the research on trans-BBB liposomes and micelles were discussed according to the current clinical translation, which may provide refe-rences and ideas for the development of trans-BBB targeted nano-drugs.

A novel polyphyllin I-based liposome delivery system sensitizes hepatic carcinoma to doxorubicin via cholesterol modulation

Cholesterol and its metabolites act as important signaling molecules that promote tumor development. In recent years, increasing evidence has indicated that targeting cholesterol biosynthesis, metabolism, and membrane distribution could potentially sensitize cancer cells to chemotherapy. However, because of the lack of selectivity and the large differences in half-life, metabolism, and clearance between drugs, combining cholesterol inhibitors with chemotherapy agents can produce toxic side effects and contradictory results, making this kind of treatment highly controversial. Here, we developed a PPI-based multifunctional liposome system to effectively cope with the above challenges. As a steroidal saponin, PPI acts as a membrane stabilizer to replace the cholesterol needed to form liposomes, avoiding the shortcomings caused by extra cholesterol intake. Moreover, as a chemotherapy adjuvant, PPI has great potential to interfere with cancer-derived cholesterol disorders, exerting a cholesterol-lowering effect as strong as lovastatin. The expression of important cholesterol synthesis-related proteins, SOAT1, HMGCR, and SREBP2, were only 1/3-1/2 of lovastatin. In addition, by forming complexes with membrane cholesterol, PPI not only improves plasma membrane fluidity and permeability but also disrupt the distribution of lipid rafts, which decreased the expression of ABC transporters to 0.6–1.0-fold, allowing more chemotherapy agents to reach the intracellular targets. Finally, PPI-DOX co-loaded liposomes (DLPs) exhibited stronger tumor inhibition effect in in vivo animal studies, which was 1.3-fold that of Chol-DOX-LP. Therefore, PPI-based liposomes offer a new strategy and opportunity for cancer treatment by combining cancer-derived cholesterol modulation with other anti-cancer therapies.

Synthesis & Evaluation of Novel Mannosylated Neoglycolipids for Liposomal Delivery System Applications.

Glycosylated NPs, including liposomes, are known to target various receptors involved in cellular carbohydrate transport, of which the mannoside binding receptors are attracting particular attention for their expression on various immune cells, cancers, and cells involved in maintaining central nervous system (CNS) integrity. As part of our interest in NP drug delivery, mannosylated glycoliposomal delivery systems formed from the self-assembly of amphiphilic neoglycolipids were developed, with a C12-alkyl mannopyranoside (ML-C12) being identified as a lead compoundcapable of entrapping, protecting, and improving the delivery of structurally diverse payloads. However, ML-C12 was not without limitations in both the synthesis of the glycolipids, and the physicochemical properties of the resulting glycoliposomes. Herein, the chemical syntheses of a novel series of mannosylated neoglycolipids are reported with the goal of further improving on the previous ML-C12 glyconanoparticles. The current work aimed to use a self-contingent strategy which overcomes previous synthetic limitations to produce neoglycolipids that have one exposed mannose residue, an aromatic scaffold, and two lipid tails with varied alkyl chains. The azido-ending carbohydrates and the carboxylic acid-ending lipid tails were ligated using a new one-pot modified Staudinger chemistry that differed advantageously to previous syntheses. The formation of stable neoglycoliposomes of controllable and ideal sizes (≈100-400 nm) was confirmed via dynamic light scattering (DLS) experiments and transmission electron microscopy (TEM). Beyond chemical advantages, the present study further aimed to establish potential improvements in the biological activity of the neoglycoliposomes. Concanavalin A (Con A) agglutination studies demonstrated efficient and stable cross-linking abilities dependent on the length of the linkers and lipid tails. The efficacy of the glycoliposomes in improving cytosolic uptake was investigated using Nile Red as probe in immune and cancer cell lines. Preliminary ex vivo safety assessments showed that the mannosylated glycoliposomes are hemocompatible, and non-immunogenic. Finally, using a model peptide therapeutic, the relative entrapment capacity and plasma stability of the optimal glycoliposome delivery system was evaluated and compared to the previous neoglycoliposomes. Overall, the new lead glycoliposome showed improved biological activity over ML-C12, in addition to having several chemical benefits including the lack of stereocenters, a longer linker allowing better sugar availability, and ease of synthesis using novel one-pot modified Staudinger chemistry.

Comparison of two methods for tumour-targeting peptide modification of liposomes.

Liposomes decorated with tumour-targeting cell-penetrating peptides can enhance specific drug delivery at the tumour site. The TR peptide, c(RGDfK)-AGYLLGHINLHHLAHL(Aib)HHIL, is pH-sensitive and actively targets tumour cells that overexpress integrin receptor αvβ3, such as B16F10 melanoma cells. Liposomes can be modified with the TR peptide by two different methods: utilization of the cysteine residue on TR to link DSPE-PEG2000-Mal contained in the liposome formula (LIPTR) or decoration of TR with a C18 stearyl chain (C18-TR) for direct insertion into the liposomal phospholipid bilayer through electrostatic and hydrophobic interactions (LIPC18-TR). We found that both TR and C18-TR effectively reversed the surface charge of the liposomes when the systems encountered the low pH of the tumour microenvironment, but LIPC18-TR exhibited a greater increase in the charge, which led to higher cellular uptake efficiency. Correspondingly, the IC50 values of PTX-LIPTR and PTX-LIPC18-TR in B16F10 cells in vitro were 2.1-fold and 2.5-fold lower than that of the unmodified PTX-loaded liposomes (PTX-LIP), respectively, in an acidic microenvironment (pH 6.3). In B16F10 tumour-bearing mice, intravenous administration of PTX-LIPTR and PTX-LIPC18-TR (8 mg/kg PTX every other day for a total of 4 injections) caused tumour reduction ratios of 39.4% and 56.1%, respectively, compared to 20.8% after PTX-LIP administration. Thus, we demonstrated that TR peptide modification could improve the antitumour efficiency of liposomal delivery systems, with C18-TR presenting significantly better results. After investigating different modification methods, our data show that selecting an adequate method is vital even when the same molecule is used for decoration.

Updates on Responsive Drug Delivery Based on Liposome Vehicles for Cancer Treatment.

Liposomes are well-known nanoparticles with a non-toxic nature and the ability to incorporate both hydrophilic and hydrophobic drugs simultaneously. As modern drug delivery formulations are produced by emerging technologies, numerous advantages of liposomal drug delivery systems over conventional liposomes or free drug treatment of cancer have been reported. Recently, liposome nanocarriers have exhibited high drug loading capacity, drug protection, improved bioavailability, enhanced intercellular delivery, and better therapeutic effect because of resounding success in targeting delivery. The site targeting of smart responsive liposomes, achieved through changes in their physicochemical and morphological properties, allows for the controlled release of active compounds under certain endogenous or exogenous stimuli. In that way, the multifunctional and stimuli-responsive nanocarriers for the drug delivery of cancer therapeutics enhance the efficacy of treatment prevention and fighting over metastases, while limiting the systemic side effects on healthy tissues and organs. Since liposomes constitute promising nanocarriers for site-targeted and controlled anticancer drug release, this review focuses on the recent progress of smart liposome achievements for anticancer drug delivery applications.

Development of Stable Liposomal Drug Delivery System of Thymoquinone and Its In Vitro Anticancer Studies Using Breast Cancer and Cervical Cancer Cell Lines

Thymoquinone, a well-known phytoconstituent derived from the seeds of Nigella sativa, exhibits unique pharmacological activities However, despite the various medicinal properties of thymoquinone, its administration in vivo remains challenging due to poor aqueous solubility, bioavailability, and stability. Therefore, an advanced drugdelivery system is required to improve the therapeutic outcome of thymoquinone by enhancing its solubility and stability in biological systems. Therefore, this study is mainly focused on preparing thymoquinone-loaded liposomes to improve its physicochemical stability in gastric media and its performance in different cancer cell line studies. Liposomes were prepared using phospholipid extracted from egg yolk. The liposomal nano preparations were evaluated in terms of hydrodynamic diameter, zeta potential, microscopic analysis, and entrapment efficiency. Cell-viability measurements were conducted using breast and cervical cancer cell lines. Optimized liposomal preparation exhibited polygonal, globule-like shape with a hydrodynamic diameter of less than 260 nm, PDI of 0.6, and zeta potential values of −23.0 mV. Solid-state characterizations performed using DSC and XRPD showed that the freeze-dried liposomal preparations were amorphous in nature. Gastric pH stability data showed no physical changes (precipitation, degradation) or significant growth in the average size of blank and thymoquinone-loaded liposomes after 24 h. Cell line studies exhibited better performance for thymoquinone-loaded liposomal drug delivery system compared with the thymoquinone-only solution; this finding can play a critical role in improving breast and cervical cancer treatment management.

INFLUENCE OF THE LIPID COMPOSITION ON THE PROPERTIES, TECHNOLOGY AND QUALITY INDICATORS OF LIPOSOMAL DRUGS

Liposomal drug delivery system is an example of the use of nanodrugs in medical practice. Encapsulation of active pharmaceutical ingredients in liposomal nanoparticles allows increasing their bioavailability and efficacy. Aim. The article is devoted to the analysis of the lipid composition of liposomal drugs developed in Ukraine, its influence on the choice of technology and control parameters. Results. The lipid compositions of liposomal drugs developed in Ukraine in recent years were reviewed. The advantages and disadvantages of natural phosphatidylcholine as the main membrane-forming lipid were analyzed. Data on the influence of anionic phospholipids and cholesterol in the liposomal membrane composition on the stability of liposomal nanoparticles and the level of active pharmaceutical ingredient encapsulation were given. The main technological stages of obtaining liposomes with hydrophilic and hydrophobic active pharmaceutical ingredients were considered. The main groups of quality indicators of liposomal dosage forms have been determined. Conclusions. The lipid composition determines the structure and physicochemical properties of the lipid membrane, the mechanism and level of active pharmaceutical ingredient encapsulation, which significantly influences the pharmacological efficacy of liposomal drug delivery systems.

Liposomal drug delivery systems for the treatment of leishmaniasis.

Human le ishmaniasis is a vector-borne, neglected infectious disease that is widely distributed in America, Africa, Europe, and Asia. Current therapy is based on old and toxic drugs, including antimonials, aminoglycosides, and amphotericin. As a neglected disease, investment in the development of new therapeutic molecules is scarce. Considering these aspects, the optimization of treatment through novel delivery systems for current therapeutic agents is an attractive alternative. The encapsulation into liposomes of drugs used in treating leishmaniasis increases the concentration of these molecules in macrophages, which may not only increase the chance of cure but also expand their therapeutic spectrum to include resistant Leishmania, as well as reducing toxicity since the drug is less exposed to healthy cells. The classical example is the liposomal formulation of amphotericin B, a well-established therapeutic option that uses liposomes to decrease the progression of renal failure in patients. However, loading other leishmanicidal drugs into liposomes, such as pentavalent antimonials, presents an opportunity for innovative and cheaper therapeutic options for the treatment of human leishmaniasis. This review aims to discuss liposomes as a drug delivery system for leishmanicidal drugs.