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This study aimed to characterize a stable nano-niosome formulation, which could reduce the adverse effects of carboplatin (CB) and improve its therapeutic efficacy in the treatment of breast cancer. For this purpose, CB-loaded polyethylene glycol (PEG)ylated niosome nanoparticles (PEG-NS-CB) were synthesized using the reverse-phase evaporation method. PEG-NS-CB (226.0 ± 10.6 nm) could release CB in a controlled manner and, compared to CB and CB-loaded non-PEGylated niosome (NS-CB), caused higher cytotoxicity effects against mouse breast cancer 4T1 cells (IC

When developing topical semisolid products, it is crucial to consider the metamorphosis of the formulation under the “in use” condition. Numerous critical quality characteristics, including rheological properties, thermodynamic activity, particle size, globule size, and the rate/extent of drug release/permeation, can be altered during this process. This study aimed to use lidocaine as a model drug to establish a connection between the evaporation and change of rheological properties and the permeation of active pharmaceutical ingredients (APIs) in topical semisolid products under the “in use” condition. The evaporation rate of the lidocaine cream formulation was calculated by measuring the weight loss and heat flow of the sample using DSC/TGA. Changes in rheological properties due to metamorphosis were assessed and predicted using the Carreau–Yasuda model. The impact of solvent evaporation on a drug’s permeability was studied by in vitro permeation testing (IVPT) using occluded and unconcluded cells. Overall, it was found that the viscosity and elastic modulus of prepared lidocaine cream gradually increased with the time of evaporation as a result of the aggregation of carbopol micelles and the crystallization of API after application. Compared to occluded cells, the permeability of lidocaine for formulation F1 (2.5% lidocaine) in unoccluded cells decreased by 32.4%. This was believed to be the result of increasing viscosity and crystallization of lidocaine instead of depletion of API from the applied dose, which was confirmed by formulation F2 with a higher content of API (5% lidocaine) showing a similar pattern, i.e., a 49.7% reduction of permeability after 4 h of study. To the best of our knowledge, this is the first study to simultaneously demonstrate the rheological change of a topical semisolid formulation during volatile solvent evaporation, resulting in a concurrent decrease in the permeability of API, which provides mathematical modelers with the necessary background to build complex models that incorporate evaporation, viscosity, and drug permeation in the simulation once at a time.

Loss or dysfunction of the pancreatic beta cells or insulin receptors leads to diabetes mellitus (DM). This usually occurs over many years; therefore, the development of methods for the timely detection and clinical intervention are vital to prevent the development of this disease. Glucagon-like peptide-1 receptor (GLP-1R) is the receptor of GLP-1, an incretin hormone that causes insulin secretion in a glucose-dependent manner. GLP-1R is highly expressed on the surface of pancreatic beta cells, providing a potential target for bioimaging. In this review, we provide an overview of various strategies, such as the development of GLP-1R agonists (e.g., exendin-4), and GLP-1 sequence modifications for GLP-1R targeting for the diagnosis and treatment of pancreatic beta cell disorders. We also discuss the challenges of targeting pancreatic beta cells and strategies to address such challenges.

Drug repositioning is defined as a process to identify a new application for drugs. This approach is critical as it takes advantage of well-known pharmacokinetics, pharmacodynamics, and toxicity profiles of the drugs; thus, the chance of their future failure decreases, and the cost of their development and the required time for their approval are reduced. Anthelmintics, which are antiparasitic drugs, have recently demonstrated promising anticancer effects in vitro and in vivo. This literature review focuses on the potential of anthelmintics for repositioning in the treatment of cancers. It also discusses their pharmacokinetics and pharmacodynamics as antiparasitic drugs, proposed anticancer mechanisms, present development conditions, challenges in cancer therapy, and strategies to overcome these challenges.

Camel milk is a valuable source of nutrition with a wide range of therapeutic effects. Its unique composition helps to regulate the blood glucose level. The current study is aimed to evaluate the antidiabetic and hepatoprotective effects, as well as lipid profile restoration of camel milk in the diabetic mouse model. This innovative study evaluates the therapeutic effects of camel milk in diabetic mice by simultaneous measurement of blood glucose, HbA1c, ALT, AST, TG, cholesterol, and histopathological studies. The results showed that camel milk has significantly reduced blood glucose, HbA1c (p, Camel milk as a natural safe product can be used as an alternative treatment regimen in diabetes therapy. Potency of camel milk is to restore the activity of hepatocyte enzymes such as ALT and AST. Camel milk is an effective approximately as much as glibenclamide to normalize blood TG and cholesterol concentrations.

Mesoporous silica nanoparticles (MSNPs) are a particular example of innovative nanomaterials for the development of drug delivery systems. MSNPs have recently received more attention for biological and pharmaceutical applications due to their capability to deliver therapeutic agents. Due to their unique structure, they can function as an effective carrier for the delivery of therapeutic agents to mitigate diseases progress, reduce inflammatory responses and consequently improve cancer treatment. The potency of MSNPs for the diagnosis and management of various diseases has been studied. This literature review will take an in-depth look into the properties of various types of MSNPs (e.g. shape, particle and pore size, surface area, pore volume and surface functionalisation), and discuss their characteristics, in terms of cellular uptake, drug delivery and release. MSNPs will then be discussed in terms of their therapeutic applications (passive and active tumour targeting, theranostics, biosensing and immunostimulative), biocompatibility and safety issues. Also, emerging trends and expected future advancements of this carrier will be provided.

This study aimed to develop and optimize chemistries to produce alkyne-modified glucagon-like peptide-1(7-36)-amide (GLP-1(7-36)-NH2) libraries, which could be rapidly and efficiently conjugated to other components and screened to identify compounds with the best drug delivery properties, as potential treatments for type 2 diabetes or obesity. For this purpose, the Lys26 (K26) side-chain, and the amino (N)- and carboxy (C)-termini of a dipeptidyl peptidase 4 (DPPIV)-resistant GLP-1 sequence (GLP-1(7-36;A8G)-NH2), were modified with an alkyne (4-pentynoic acid or propiolic acid). These analogs were characterized with respect to human GLP-1 receptor (hGLP-1R) agonist activity, effects on cell viability and human serum stability, revealing that these modifications maintained low (N-terminal; EC50 1.5 × 10-9 M) to subnanomolar (C-terminal and K26, ∼4 × 10-10 M) agonist activity toward hGLP-1, had no effect on cell viability, and for the N-terminal and K26 modifications, increased human serum proteolytic stability (t1/2 > 24 h). Copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction conditions were investigated using the C-terminal modified GLP-1 analog and an azide-modified model lipid peptide, with respect to the effects of altering the azide/alkyne ratio, cosolvents, temperature, reducing agents, Cu(I)-stabilizing ligand, copper source, and the concentrations of reagents/reactants, in order to identify general conditions that provide fast reactions and high yields. A 1:2 azide-alkyne (lipid:GLP-1 peptide) and 4:1 sodium ascorbate/copper sulfate molar ratio in 65% v/v DMSO-water at room temperature, in the absence of Cu(I)-stabilizing ligands (THPTA or l-histidine) and buffers (phosphate, pH 7), provided the best yields. This work reports a library of characterized GLP-1 analogs and chemistries for their attachment to other species, providing useful tools to improve GLP-1 delivery and pharmacology (e.g., through conjugation to other species that lower blood glucose, increase the duration of action, or enable delivery via a nonparenteral route).

Staphylococcus aureus (S. aureus) biofilm-associated infections are a primary concern for public health worldwide. Current therapeutics cannot penetrate the biofilms efficiently, resulting in low drug concentrations at the infected sites and increasing the frequency of drug usage. To solve this issue, nanotechnology platforms seem to be a promising approach. In this study, the potential therapeutic effects of (PEG)ylated liposome (PEG-Lip) for the delivery of nafcillin (NF) antibiotic were assessed. The results demonstrated that NF-loaded liposome (Lip-NF) and NF-loaded PEG-Lip (PEG-Lip-NF) released 76.4 and 62% of the loaded NF, respectively, in a controlled manner after 50 h. Also, it was found that PEG-Lip-NF, compared to Lip-NF and NF, was more effective against a methicillin-susceptible S. aureus (MSSA; minimum inhibitory concentration (MIC): 1.0 ± 0.03, 0.5 ± 0.02, and 0.25 ± 0.01 μg/mL; and minimum biofilm inhibitory concentration (MBIC

The present study aimed to synthesize albendazole (ABZ)-loaded Mobil Composition of Matter No. 41 (MCM-41 NPs) to increase the efficacy of the drug against liver cancer. ABZ was loaded into MCM-41 NPs, and after

Tumor necrosis factor receptor 1 (TNFR1) is expressed on tumor cells and induces cell apoptosis through triggering proapoptotic cascade in these cells. Agonist antibodies specific for TNFR1 mimic the role of receptor ligands and can induce apoptosis in tumor cells. This study aims to prepare cysteine-rich domain2 (CRD2) and CRD3 of the extracellular region of TNFR1 receptor as a recombinant protein, and encapsulate the protein into pegylated liposomal nanoparticles to obtain an adjuvant antigen for cancer treatment. In this study, the size, size distribution and zeta potential of particles were determined by Zetasizer, and their stability was evaluated after 3 months of their production time. Moreover, the adjuvant effect of liposomal nanoparticles was evaluated in an in vitro environment using dendritic and lymphocyte cells. The size and zeta potential of protein-loaded pegylated liposomal nanoparticles were 274 ± 13 nm and − 28 mV, respectively, with 78% ± 2.3 protein encapsulation efficiency. In addition, the adjuvant effect of liposomal nanoparticles as the recombinant protein carrier was confirmed, in which the lymphocyte proliferation was increased by 1.5-fold in the presence of liposomal nanoparticles. The results of the present study suggest that CRD2 and CRD3 encapsulated into pegylated liposomal nanoparticles can be used as adjuvant antigens for the production of specific agonist antibody for TNFR1 stimulation in an in vivo environment.

Glucagon-like peptide-1 GLP-1 is a gut-derived peptide secreted from pancreatic β-cells that reduces blood glucose levels and body weight; however, native GLP-1 (GLP-1(7-36)-NH2 and GLP-1(7-37)) have short in vivo circulation half-lives (∼2 min) due to proteolytic degradation and rapid renal clearance due to its low molecular weight (MW; 3297.7 Da). This study aimed to improve the proteolytic stability and delivery properties of glucagon-like peptide-1 (GLP-1) through modifications that form nanostructures. For this purpose, N- (NtG) and C-terminal (CtG), and Lys26 side chain (K26G) alkyne-modified GLP-1 analogues were conjugated to an azide-modified lipidic peptide (L) to give N-L, C-L, and K-26-L, respectively; or CtG was conjugated with a fibrilizing self-assembling peptide (SAP) (AEAEAKAK)3 to yield C-S, using copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC). N-L demonstrated the best serum stability (t1/2 > 48 h) compared to K-26-L (44 h), C-L (20 h), C-S (27 h), and the parental GLP-1(7-36;A8G)-NH2 (A8G) (19 h) peptides. Each conjugate demonstrated subnanomolar hGLP-1RA potency, and none demonstrated toxicity toward PC-3 cells at concentrations up to 1 μM. Each analogue was observed by transmission electron microscopy to form fibrils in solution. K-26-L demonstrated among the best human serum stability (t1/2 = 44 h) and similar hGLP-1RA potency (EC50 48 pM) to C-S. In conclusion, this study provided an alternative to lipid modification, i.e., fibrillizing peptides, that could improve pharmacokinetic parameters of GLP-1.

The present study aimed to synthesize albendazole (ABZ)-loaded Mobil Composition of Matter No. 41 (MCM-41) nanoparticles (NPs) to increase the efficacy of the drug against liver cancer. ABZ was loaded into MCM-41 NPs, and after in vitro characterization, such as size, size distribution, zeta potential, morphology, chemical composition, thermal profile, drug release, surface and pore volume, and pore size, their biological effects were evaluated using 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) cell migration assays. The results demonstrated that monodispersed and spherical NPs with a size of 220 ± 11.5 and 293 ± 8.7 nm, for MCM-41 NPs and ABZ-loaded MCM-41 NPs, respectively, and drug loading efficiency of 30% were synthesized. ABZ was loaded physically into MCM-41 NPs, leading to a decrease in surface volume, pore size, and pore volume. Also, MCM-41 NPs could increase the cytotoxicity effects of ABZ by 2.9-fold (IC50 = 23 and 7.9 µM for ABZ and ABZ-loaded MCM-41 NPs, respectively). In addition, ABZ-loaded MCM-41 NPs, compared to that of ABZ, caused a significant decrease in cell migration. Overall, the results of the present study suggest evaluating the potency of MCM-41 NPs, as a potent nanoplatform, for ABZ delivery in vivo environment.

Herein, a multi-functional nano-in-micro hierarchical microsphere system is demonstrated for controlling the intestinal efflux pumps that affect the oral bioavailability of many therapeutic drugs. The hierarchical particles were generated by a co-flow microfluidic device and consisted of porous silica nanoparticles packed in Eudragit® polymeric matrix. Meropenem (MER), a last-resort antibacterial drug, was loaded into porous silica (MCM-48) with a loading capacity of 34.3 wt%. In this unique materials combination, MCM-48 enables ultrahigh loading of a hydrophilic MER, while the Eudragit® polymers not only protect MER from gastric pH but also act as an antagonist for p-glycoprotein protein efflux pumps to reduce the efflux of MER back into the gastrointestinal lumen. We investigated the in-vitro temporal MER release and bidirectional (absorptive and secretory) drug permeation model across the Caco-2 monolayer. The bioavailability of MER was significantly improved by all of the prepared formulations (i.e. increased absorptive transport and reduced secretory transport). The Eudragit® RSPO formulated MER-MCM showed the best performance with an efflux ratio (i.e. secretory transport/absorptive transport) of 0.35, which is 7.4 folds less than pure MER (2.62). Lastly, the prepared formulations were able to retain the antibacterial activity of MER against Staphylococcus aureus and Pseudomonas aeruginosa. Statement of significance Meropenem (MER) is a last resort antibiotic used for the treatment of drug-resistant and acute infections and only available as intravenous injectable dosage due to its poor chemical and thermal stability, and ultra-poor oral bioavailability because of the efflux action of P-glycoprotein (P-gp) pumps. Multifunctional colloidal micro/nanoparticles can help to solve these issues. Herein, we designed pomegranate-like hierarchical microspheres comprised of porous silica nanoparticles and enteric Eudragit® polymers (Eudragit®S100, Eudragit®RSPO, and Eudragit®RS100) using a co-flow microfluidic device. Our formulations allow for ultrahigh loading of hydrophilic MER, protects MER from gastric pH, and also block P-gp efflux pumps for enhanced MER permeation/retention with Eudragit®RSPO – showing 13.9-folds higher permeation and 7.4-folds reduction in efflux ratio in a bi-directional Caco-2 monolayer culture system.

The crucial functions of chemokine/receptors in numerous parasitic infections, including leishmaniasis, are well documented. This study aimed to assess the serum levels of CC ligand (CCL) 2, CCL5, and CCL11 in cutaneous leishmaniasis (CL) patients. 64 patients, suffering from CL and 100 healthy people were selected, and their blood serum concentrations of CCL2, CCL5, and CCL11 were measured using enzyme-linked immunosorbent assay. The results demonstrated that while the mean serum levels of CCL5 and CCL11 increased significantly in CL patients, the mean serum levels of CCL2 decreased, compared to the control group. Despite the sufficient production of CCL5 and CCL11 in CL patients, they suffered from CCL2 deficiency, as the defense mechanism against parasitic infection. These findings suggest a mechanism that might partially explain the patients’ susceptibility to persistent infection and their inability to clear the parasites.

This study aims to evaluate the potency of cisplatin (Cispt)-loaded liposome (LCispt) and PEGylated liposome (PLCispt) as therapeutic nanoformulations in the treatment of bladder cancer (BC). Cispt was loaded into liposomes using reverse-phase evaporation method, and the formulations were characterized using dynamic light scattering, scanning electron microscopy, dialysis membrane, and Fourier-transform infrared spectroscopy (FTIR) methods. The results showed that the particles were formed in spherical monodispersed shapes with a nanoscale size (221&ndash, 274 nm) and controlled drug release profile. The cytotoxicity effects of LCispt and PLCispt were assessed in an in vitro environment, and the results demonstrated that PLCispt caused a 2.4- and 1.9-fold increase in the cytotoxicity effects of Cispt after 24 and 48 h, respectively. The therapeutic and toxicity effects of the formulations were also assessed on BC-bearing rats. The results showed that PLCispt caused a 4.8-fold increase in the drug efficacy (tumor volume of 11 &plusmn, 0.5 and 2.3 &plusmn, 0.1 mm3 in Cispt and PLCispt receiver rats, respectively) and a 3.3-fold decrease in the toxicity effects of the drug (bodyweight gains of 3% and 10% in Cispt and PLCispt receiver rats, respectively). The results of toxicity were also confirmed by histopathological studies. Overall, this study suggests that the PEGylation of LCispt is a promising approach to achieve a nanoformulation with enhanced anticancer effects and reduced toxicity compared to Cispt for the treatment of BC.

This study aimed to evaluate the cytotoxicity effects of various polyethylene glycols (PEGs), and construction and characterization of polybutylcyanoacrylate (PBCA) nanoparticles. Cytotoxicity was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay on rat glioma C6 cell line, and PBCA nanoparticles were prepared by emulsion polymerization method. Also, the nanoparticles were characterized by dynamic light scattering and scanning electron microscopy. The findings showed that PEGs were approximately safe and cytotoxicity was inversely proportional with their molecular weights. In addition, the size of nanoparticles were increased with reducing molecular weights of PEGs. PEGs with negligible cytotoxicity and stabilizing functionality were demonstrated in this study.

This study aims to prepare, characterize and evaluate the pharmacokinetics of liposomal donepezil HCl (LDH) dispersed into thiolated chitosan hydrogel (TCH) in rabbits. Various hydrogels including TCH were prepared, and after characterization, TCH was selected for subsequent evaluations, due to the promising results. TCH was then incorporated with LDH prepared by reverse phase evaporation method. The hydrogel was characterized using scanning electron microscope, dialysis membrane technique, and ultra-performance liquid chromatography methods. The optimized resultant was then evaluated in terms of pharmacokinetics in an in vivo environment. The mean size of LDH and drug entrapment efficiency were 438.7 ± 28.3 nm and 62.5% ± 0.6, respectively. The controlled drug release pattern results showed that the half-life of the loaded drug was approximately 3.5 h. Liposomal hydrogel and free liposomes were more stable at 4 °C compared to those in 20 °C. The pharmacokinetics study in the rabbit showed that the optimized hydrogel increased the mean peak drug concentration and area under the curve by 46% and 39%, respectively, through nasal route compared to the oral tablets of DH. Moreover, intranasal delivery of DH through liposomal hydrogel increased the mean brain content of the drug by 107% compared to the oral DH tablets. The results suggested that liposomes dispersed into TCH is a promising device for the nasal delivery of DH and can be considered for the treatment of Alzheimer’s disease.

Type 2 diabetes mellitus (T2DM) is increasing in global prevalence and is associated with serious health problems (e.g., cardiovascular disease). Various treatment options are available for T2DM, including the incretin hormone glucagon-like peptide-1 (GLP-1). GLP-1 is a therapeutic peptide secreted from the intestines following food intake, which stimulates the secretion of insulin from the pancreas. The native GLP-1 has a very short plasma half-life, owning to renal clearance and degradation by the enzyme dipeptidyl peptidase-4. To overcome this issue, various GLP-1 agonists with increased resistance to proteolytic degradation and reduced renal clearance have been developed, with several currently marketed. Strategies, such as controlled release delivery systems, methods to reduce renal clearance (e.g., PEGylation and conjugation to antibodies), and methods to improve proteolytic stability (e.g., stapling, cyclization, and glycosylation) provide means to further improve the ability of GLP-1 analogs. These will be discussed in this literature review.

This study aims to improve the cytotoxicity and potency of cisplatin-loaded polybutylcyanoacrylate (PBCA) nanoparticles (NPs) for the treatment of lung cancer through the modulation of temperature and polyethylene glycol (PEG) concentration as effective factors affecting the NPs&rsquo, properties. The NPs were synthesized using an anionic polymerization method and were characterized in terms of size, drug loading efficiency, drug release profile, cytotoxicity effects, drug efficacy, and drug side effects. In this regard, dynamic light scattering (DLS), scanning electron microscopy (SEM), 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) methods, and hematoxylin and eosin (H&amp, E) staining were used. The results showed that the size and the drug loading efficiency of the synthesized spherical NPs were 355&ndash, 386 nm and 14&ndash, 19%, respectively. Also, the drug release profile showed a controlled and slow drug release pattern with approximately 10% drug release over 48 h. In addition, the NPs significantly increased the cytotoxicity of the cisplatin in vitro environment by approximately 2 times and enhanced the therapeutic effects of the drug in vivo environment by increasing the survival time of lung-cancer-bearing mice by 20% compared to the standard drug receiver group. Also, the nanoformulation decreased the drug toxicity in an in vivo environment. According to the results, increasing the temperature and PEG concentration improved the properties of the drug loading efficiency, drug release profile, and cytotoxicity effect of drug-loaded NPs. Consequently, the synthesized formulation increased the survival of tumor-bearing mice and simultaneously decreased the cisplatin toxicity effects. In conclusion, the prepared nanoformulation can be considered a promising candidate for further evaluation for possible therapeutic use in the treatment of lung cancer.

Breast cancer is the most common cancer and the second cause of cancer-related death in women worldwide. Chemotherapy of disease is impeded by subsequent relapse and metastasis. Nanoparticles as drug carriers have been shown the promising results. Cisplatin-loaded polybutylcyanoacrylate (PBCA) nanoparticles (NPs) were successfully constructed, and its efficacy and toxicity were evaluated on an orthotopic breast cancer model. Cisplatin-loaded PBCA NPs were prepared by miniemulsion polymerization technique. NPs were characterized with photon correlation spectroscopy, inductively coupled plasma optical emission spectrometry (ICP-OES) and spectrophotometry techniques. MTT assay was used to evaluate the cytotoxicity of nanodrug. To evaluate the efficacy of Cisplatin-loaded PBCA NPs an orthotopic model of breast tumor was employed. The cell viability of nanodrug compared to that of the standard drug had a significant decrease by 75% at the first 24 h. In vivo studies showed that the number of mice treated with Cisplatin bound to PBCA NPs was significantly more than the standard drug receivers (8 against 5 mice). Considering the body weight loss as toxicity effects, nanodrug receivers were also shown significantly lesser body weight loss compared to drug receivers groups (20 against 26%).

Bipolar disorder is a chronic mental illness which is associated with high risk of self-harm and suicide. Lithium carbonate has been suggested as a medicine to control and cure this disease. To overcome the complications related to taking lithium carbonate, nanotechnology has come to the aid of scientists. In this study, pegylated liposomal lithium carbonate nanoparticles were prepared by the reverse phase evaporation method to improve the drug’s therapeutic characteristics as well as lessening its side effects. In order to synthesize pegylated liposomal lithium carbonate, phosphatidylcholine, polyethylene glycol 3350 (PEG3350), cholesterol, and lithium carbonate were mixed. The characterization of synthesized nanoparticles was determined by Zetasizer. Encapsulation and drug loading efficiency and release pattern studies were determined through spectrophotometry method. In addition, serum lithium and creatinine levels of the samples were analyzed. The mean diameter, size distribution, and zeta potential for pegylated liposomal particles containing lithium carbonate and blank pegylated liposomal were determined by Zetasizer equal to 102 nm, 0.458, and −25.1 mV; 284.2 nm, 0.427, and −28.3 mV, respectively. Drug loading and encapsulation efficiency were calculated to be 32.87 and 97.4 %, respectively. The drug release pattern demonstrated that the half-life of the nanodrug was approximately two times higher than the standard drug. The results related to the analysis of serum lithium and creatinine levels indicated that the efficiency of liposomal drug formulation was increased compared to the standard drug. Based on the findings, the nanodrug enjoyed a half-life two times higher than that of the standard drug and an efficiency level equal to it.

One of the main challenges of treatment of ovarian cancer is initial response to treatment and then acquisition of resistance to Cisplatin. Nanotechnology-based approaches are considered as one way to overcome drug resistance. In this study, the cytotoxicity effects of Cisplatin-loaded poly butyl cyanoacrylate (PBCA) nanoparticles (NPs) on the ovarian cancer cell line A2780cp resistant to Cisplatin were studied. NPs were synthesized by miniemulsion polymerization method. Size, size distribution and zeta potential of NPs were estimated as 489 nm, 0.429, and -20 mV, respectively. Drug loading and encapsulation efficiency were recognized as 5 % and 25 %, respectively. Drug release pattern (3.18 % release after 51 h) demonstrated high level of retention. Toxicological studies showed that cytotoxicity of the nanodrug Cisplatin was about three times as much as that of a free drug. Moreover, NPs presented acceptable stability after 2 months. The results of study suggest the use of this formulation for in vivo experiments.

Glioblastoma is known as one of the most aggressive human cancers. To gain access of the brain, therapeutic agents must overcome blood–brain barrier (BBB). In this study, Cisplatin (Cispt)-loaded polybutylcyanoacrylate (PBCA) nanoparticles (NPs) were prepared through miniemulsion polymerization technique. They were coated with polysorbate 80 to cross the BBB of glioblastoma-bearing rats. Prepared NPs were characterized with respect to their size, size distribution, zeta potential, drug loading and encapsulation efficiency, cytotoxicity effects, drug release, and stability pattern. Size and zeta potential of nanodrug were found to be 489 nm and −20 mV, while drug loading and encapsulation efficiency were determined to be 5 % and 25 %, respectively. Release studies demonstrated high retention capability of nanodrug in that 3.18 % of Cispt was released from NPs in a period of 51 h. NPs presented acceptable stability after 2 months and lyophilization. Mean survival time in nanodrug receivers was 19.6 days, while it was 17.5 days for free drug receivers. Histological studies demonstrated efficacy of PBCA NPs in reducing side effects. Finally, such preparation can be considered as a promising nanocarrier for other types of tumor.

New hopes in cancer treatment have been emerged using functional nanoparticles. In this work, we tried to synthesize gold nanoparticles and gold nanoparticles conjugated with DNA extracted from human breast cancer cells. After synthesizing, gold nanoparticles were mixed with nanoliposomal hydroxyurea and corresponding compounds were formed. They were described by UV–Visible spectrophotometry and Zeta sizer. Amount of drug loading into liposomes was determined by spectrophotometry and cytotoxicity effect on MCF-7 cells was measure by MTT assay. Drug loading was determined to be 70 %. Size, size distribution and Zeta potential of particles were 473 nm, 0.46 and −21 mV for control nanoliposomal ones and 351 nm, 0.38 and −25 mV for nanoliposomal particles containing hydroxyurea. This was 29 nm, 0.23 and −30 mV for gold nanoparticles and 502 nm, 0.41 and −38 mV for nanoliposomes containing drug loaded by gold nanoparticles conjugated with DNA. It was found that nano conjugated complex in concentrations less than 20 μM of hydroxyurea can improve efficiency compared with liposomal drug. In maximum concentration of drug (2,500 μM), cytotoxicity was equal to 95 %. In minimum concentration of drug (5 μM), cytotoxicity of liposomal drug and conjugated complex were 70 and 81 %, respectively which probably comes from increased drug entry into cells due to the presence of gold nanoparticles. Free drug resulted in toxicity of 32 % in 5 μM and 88 % in 2,500 μM. Results demonstrated higher drug efficiency in nanoparticle form compared with free form which can be used in in vivo studies.

Breast cancer is one of the most frequent cancer types within women population. Hydroxyurea (HU) is a chemotherapy compound for treatment of patients with cancer diagnosis, including breast cancer associated with several adverse effects. In this study, we applied nanotechnology to decreased drug side effects along with improvement of therapeutic index. Liposomation is widely used in modern pharmacological developments in order to enhance the effects of the drugs. To achieve this, in this study a mixture of phosphatidylcholine and cholesterol was made up and HU was added to the resultant mixture, was then pegylated using Polyethylene Glycol 2000 to increase resistance, applicability and solubility. The mean diameters of nanoliposomal and pegylated nanoliposomal HU were measured by Zeta sizer device and obtained about 402.5 and 338.2 nm. The efficiency of non-pegylated and pegylated liposomal HU was 70.8 and 64.2, respectively. Releasing HU in both formulations was estimated about 25.8 and 21.7 %. Also, this study investigated the cytotoxicity effect of nanoliposomal and pegylated nanoliposomal HU using MTT assay. Results of this investigation showed that the cytotoxic properties of pegylated HU was 3.6 % more than those non-pegylated form, while was 38.93 % more than ordinary from of HU. This study showed that the stability, releasing pattern and cytotoxicity of the pegylated nanoliposomal HU is better than that of nanoliposomal HU.

In the present study, paclitaxel was archaeosomed to reduce side effects and improve its therapeutic index. Carriers have made a big evolution in treatment of many diseases in recent years. Lipid carriers are of special importance among carriers. Archaeosome is one of the lipid carriers. Paclitaxel is one of the drugs used to treat breast cancer which has some unwanted side effects despite its therapeutic effects. Archaeosomes were extracted from methanogenic archi bacteria and synthesized with a certain ratio of paclitaxel in PBS. The mean diameter of archaeosomal paclitaxel was measured by Zeta sizer instrument, Drug releasing of archaeosomal paclitaxel was examined within 26 h which results showed that the most drug releasing occurs during first 3 h. The cytotoxicity effect of archaeosomal paclitaxel on breast cancer’s cell line was evaluated by MTT assay which results showed that the cytotoxicity effect of archaeosomal paclitaxel on breast cancer’s cell line is more than that of the standard paclitaxel formulation. The results indicated that new drug delivery of paclitaxel using archaeosome, increases the therapeutic index of the drug.

It is clear that cancer is one of the most mortal diseases in the world and the most prevalent among women is breast cancer. As hydroxyurea (HU)—a drug which is used in chemotherapy—has many adverse effects in long-term despite of its therapeutic properties, we made use of nano drug delivery technology in order to reduce adverse effects and increase therapeutic index. Thus, liposomation is a novel way in drug delivery systems. In this study a mixture of phosphatidylcholine and cholesterol was mixed and HU was added to the resultant mixture. The mean diameter of the nanoliposomal HU measured with the Zeta Sizer device (equal to 402.5 nm) and its encapsulation efficiency was 70.8 %. Besides, using dialysis, the pattern of drug release from nanoliposomes has been studied and the results showed that the drug release of nanoliposomal drug within 28 h was equal to 25.85 %. This study showed that the cytotoxicity effect of nanoliposomal drug is more than that of the standard drug.

Nano carriers have greatly revolutionized the treatment of most diseases recently. One of these nano carriers, liposomes, has got particular significance. On the other hand, Artemisinin which is used as an effective anticancer drug has some side effects. To reduce such side effects, liposomes can be employed. In order to prepare pegylated nanoliposomal artemisinin, particular proportions of phosphatidylcholine, polyethylene glycol 2000 and artemisinin were combined. As a result, the mean diameter of nano liposomes is 455 nm. Besides, the encapsulation efficiency and the drug release from pegylated nanoliposomes for pegylated nanoliposomal artemisinin are respectively 91.62 ± 3.5 and 5.17 %. The results also show that IC50 of the produced formulation is less than that of the standard drug. This study reveals that the amount of artemisinin cytotoxicity compared to standard drug is increased by pegylated nanoliposomal formulation.

Regarding that the breast cancer is the most prevalent disease among women, paclitaxel, an anti-cancer drug, could be used in treatment of this disease. As paclitaxel has adverse effects, it was used of nanoliposome drug delivery technology in order to reduce adverse effects and improve drug efficacy. Certain ratios of phosphatidylcholine, cholesterol and paclitaxel were synthesized to prepare nanoliposomal paclitaxel. Using Zeta sizer device, the mean diameter of nanoliposomal paclitaxel was obtained 421.4 nm and its encapsulation efficiency was 91.3 %. By dialysis, drug release in nanoliposome paclitaxel formulation within 28 h was studied which was 5.53 %. This study showed that cytotoxicity effect of nanoliposomal paclitaxel is more than that of the standard form.

Purpose : To encapsulate paclitaxel into nanoliposomes, followed by pegylatation, in order to improve its therapeutic index and reduce side effects in breast cancer. Methods : In order to prepare nanoliposomal paclitaxel, varying ratios of phosphatidylcholine, cholesterol and paclitaxel were mixed and the formulations pegylated with poly-ethylene glycol 2000 (PEG 2000) to enhance stability, efficiency, as well as solubility. The mean diameter of nanoliposomal paclitaxel and pegylated nanoliposomal paclitaxel were measured by Zeta sizer device and release of paclitaxel from both formulations was determined within 28 h by dialysis method. The cytotoxicity of nanoliposomal and pegylated nanoliposomal paclitaxel was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results : The mean diameter of nanoliposomal paclitaxel and pegylated nanoliposomal paclitaxel was 421.4 and 369.1 nm, respectively, while encapsulation efficiency was 91.3 ± 5.7 and 95.2 ± 6.3 %, respectively. Paclitaxel released from both formulations in 28 h was 5.53 and 5.02 %, respectively. The cytotoxicity of pegylated nanoliposomal paclitaxel was significantly (p . 0.05) greater than that of nanoliposomal paclitaxel (their IC50 = 79.8±2.9 and 86.25±3.4 µg/ml, respectively). Conclusion : The release pattern and cytotoxicity of pegylated nanoliposomal paclitaxel show that the formulation is superior to nanoliposomal paclitaxel. Furthermore, the mean particle size of pegylated nanoliposome is smaller than that of the non-pegylated preparation. Keywords : Paclitaxel, Nanoliposome, Breast cancer, Pegylation, Drug delivery, Cytotoxicity