Advances in nanotechnology for improving the targeted delivery and activity of amphotericin B (2011-2023): a systematic review.

Amphotericin B (AmB) is a broad-spectrum therapeutic and effective drug, but it has serious side effects of toxicity and solubility. Therefore, reducing its toxicity should be considered in therapeutic applications. Nanotechnology has paved the way to improve drug delivery systems and reduce toxicity. The present study, for the first time, comprehensively reviews the studies from 2011 to 2023 on reducing the in vitro toxicity of AmB. The findings showed that loading AmB with micellar structures, nanostructured lipid carriers, liposomes, emulsions, poly lactide-co-glycolide acid, chitosan, dendrimers, and other polymeric nanoparticles increases the biocompatibility and efficacy of the drug and significantly reduces toxicity. In addition, modified carbon nanoparticles (including graphene, carbon nanotubes, and carbon dots) with positively charged amine groups, PEI, and other components showed favorable drug delivery properties. Uncoated and coated magnetic nanoparticles and silver NPs-AmB composites had less cytotoxicity and more antifungal activity than free AmB. Citrate-reduced GNPs and lipoic acid-functionalized GNPs were also effective nanocarriers to reduce AmB cytotoxicity and improve anti-leishmania efficacy. In addition, zinc oxide-NPs and PEGylated zinc oxide-NPs showed favorable antifungal activity and negligible toxicity. According to a review study, carbon-based nanoparticles, metal nanoparticles, and especially polymer nanoparticles caused some reduction in the toxicity and improved solubility of AmB in water. Overall, considering the discussed nanocarriers, further research on the application of nanotechnology as a cost-effective candidate to improve the efficiency and reduce the cytotoxicity of AmB is recommended.

Microfluidics for personalized drug delivery.

This review highlights the transformative impact of microfluidic technology on personalized drug delivery. Microfluidics addresses issues in traditional drug synthesis, providing precise control and scalability in nanoparticle fabrication, and microfluidic platforms show high potential for versatility, offering patient-specific dosing and real-time monitoring capabilities, all integrated into wearable technology. Covalent conjugation of antibodies to nanoparticles improves bioactivity, driving innovations in drug targeting. The integration of microfluidics with sensor technologies and artificial intelligence facilitates real-time feedback and autonomous adaptation in drug delivery systems. Key challenges, such as droplet polydispersity and fluidic handling, along with future directions focusing on scalability and reliability, are essential considerations in advancing microfluidics for personalized drug delivery.

Revolutionizing Wound Healing: Exploring Scarless Solutions through Drug Delivery Innovations.

Human skin is the largest organ and outermost surface of the human body, and due to the continuous exposure to various challenges, it is prone to develop injuries, customarily known as wounds. Although various tissue engineering strategies and bioactive wound matrices have been employed to speed up wound healing, scarring remains a significant challenge. The wound environment is harsh due to the presence of degradative enzymes and elevated pH levels, and the physiological processes involved in tissue regeneration operate on distinct time scales. Therefore, there is a need for effective drug delivery systems (DDSs) to address these issues. The objective of this review is to provide a comprehensive exposition of the mechanisms underlying the skin healing process, the factors and materials used in engineering DDSs, and the different DDSs used in wound care. Furthermore, this investigation will delve into the examination of emergent technologies and potential avenues for enhancing the efficacy of wound care devices.

Bioresponsive drug delivery systems.

In this review, we highlight the potential of stimuli-responsive drug delivery systems (DDSs) to revolutionize healthcare. Through examining pH, temperature, enzyme, and redox responsiveness, the presented case studies highlight the precision and enhanced therapeutic outcomes achievable with these innovative systems. Challenges, such as complex design and bio-based material optimization, underscore the complete journey from bench to bedside. Clinical strides in magnetically and temperature-responsive systems hint at a promising future for healthcare. However, overcoming issues of stability, durability, penetration depth, sensitivity, and active targeting is crucial. The future envisions theranostic systems, amalgamating targeted therapy and diagnosis, for personalized healthcare. Bio-based materials emerge as pivotal, offering a nuanced approach to complex diseases, such as cancer and diabetes, reshaping the healthcare landscape.

Biocomposite-based strategies for dental bone regeneration.

OBJECTIVE: Because of the anatomical complexity of the oral and maxillofacial sites, repairing bone defects in these regions is very difficult. This review article aims to consider the application of biocomposites-based strategies for dental bone regeneration. STUDY DESIGN: Research papers related to the topic, published over the last 20 years, were selected using the Web of Science, Pubmed, Scopus, and Google Scholar databases. RESULTS: The strategies of monophasic, biphasic/multiphasic scaffolds, and biopolymer-based nanocomposite scaffolds containing nanomaterials compared with traditional methods used for bone regeneration, such as autografts, allografts, xenografts, and alloplasts are found to be superior because of their ability to overcome the issues (e.g., limited bone sources, pain, immune responses, high cost) related to the applications of the traditional methods. CONCLUSIONS: In addition, additive manufacturing technologies were found to be highly advantageous for improving the efficacy of biocomposite scaffolds for treating dental bone defects.

Advanced Drug Delivery Platforms for the Treatment of Oral Pathogens.

The oral cavity is a complex ecosystem accommodating various microorganisms (e.g., bacteria and fungi). Various factors, such as diet change and poor oral hygiene, can change the composition of oral microbiota, resulting in the dysbiosis of the oral micro-environment and the emergence of pathogenic microorganisms, and consequently, oral infectious diseases. Systemic administration is frequently used for drug delivery in the treatment of diseases and is associated with the problems, such as drug resistance and dysbiosis. To overcome these challenges, oral drug delivery systems (DDS) have received considerable attention. In this literature review, the related articles are identified, and their findings, in terms of current therapeutic challenges and the applications of DDSs, especially nanoscopic DDSs, for the treatment of oral infectious diseases are highlighted. DDSs are also discussed in terms of structures and therapeutic agents (e.g., antibiotics, antifungals, antiviral, and ions) that they deliver. In addition, strategies (e.g., theranostics, hydrogel, microparticle, strips/fibers, and pH-sensitive nanoparticles), which can improve the treatment outcome of these diseases, are highlighted.

Impact of PEGylated Liposomal Doxorubicin and Carboplatin Combination on Glioblastoma.

Glioblastoma is an incurable cancer with a 5-year survival chance of less than 5%. Chemotherapy is a therapeutic approach to treating the disease; however, due to the presence of the blood-brain barrier (BBB), the probability of success is low. To overcome this issue, nanoparticles are promising carriers for crossing the BBB and delivering drugs to the tumor. In this study, the anticancer efficacy of doxorubicin (DOX) and carboplatin (CB) loaded into polyethylene glycol (PEG)ylated liposome nanoparticles (PEG-Lip) and in treating brain cancer was evaluated in vitro and in vivo. The results demonstrated that PEG-Lip-DOX/CB with a size of 212 ± 10 nm was synthesized that could release the loaded drugs in a controlled manner, from which 56.3% of the loaded drugs were released after 52 h. In addition, PEG-Lip-DOX/CB could significantly increase the cytotoxicity effects of the drugs against rat glioma C6 cells (IC50: 8.7 and 12.9 µM for the drugs-loaded nanoparticles and DOX + CB, respectively). The in vivo results also demonstrated that PEGylated liposomes, compared to non-PEGylated liposomes (Lip) and DOX + CB, were more efficient in increasing the therapeutic effects and decreasing the side effects of the drugs, in which the survival times of the glioblastoma-bearing rats were 39, 35, and 30 days in the PEG-Lip-DOX/CB, Lip-DOX/CB, and DOX + CB receiver groups, respectively. In addition, the weight loss was found to be 8.7, 10.5, and 13%, respectively, in the groups. The results of the toxicity evaluation were also confirmed by histopathological studies. Overall, the results of this study demonstrated that the encapsulation of DOX and CB into PEG-Lip is a promising approach to improving the properties of DOX and CB in terms of their therapeutic effects and drug side effects for the treatment of glioblastoma.

A PEGylated Nanostructured Lipid Carrier for Enhanced Oral Delivery of Antibiotics.

Antimicrobial resistance is a major concern for public health throughout the world that severely restricts available treatments. In this context, methicillin-resistant Staphylococcus aureus (MRSA) is responsible for a high percentage of S. aureus infections and mortality. To overcome this challenge, nanoparticles are appropriate tools as drug carriers to improve the therapeutic efficacy and decrease the toxicity of drugs. In this study, a polyethylene glycol (PEG)ylated nanostructured lipid carrier (PEG-NLC) was synthesized to improve the oral delivery of trimethoprim/sulfamethoxazole (TMP/SMZ) for the treatment of MRSA skin infection in vitro and in vivo. The nanoformulation (PEG-TMP/SMZ-NLC) was synthesized with size and drug encapsulation efficiencies of 187 ± 9 nm and 93.3%, respectively, which could release the drugs in a controlled manner at intestinal pH. PEG-TMP/SMZ-NLC was found efficient in decreasing the drugs' toxicity by 2.4-fold in vitro. In addition, the intestinal permeability of TMP/SMZ was enhanced by 54%, and the antibacterial effects of the drugs were enhanced by 8-fold in vitro. The results of the stability study demonstrated that PEG-TMP/SMZ-NLC was stable for three months. In addition, the results demonstrated that PEG-TMP/SMZ-NLC after oral administration could decrease the drugs' side-effects such as renal and hepatic toxicity by ~5-fold in MRSA skin infection in Balb/c mice, while it could improve the antibacterial effects of TMP/SMZ by 3 orders of magnitude. Overall, the results of this study suggest that the application of PEGylated NLC nanoparticles is a promising approach to improving the oral delivery of TMP/SMZ for the treatment of MRSA skin infection.

Carboplatin Niosomal Nanoplatform for Potentiated Chemotherapy.

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 (IC50: 83.4, 26.6, and 22.5 µM for CB, NS-CB, and PEG-NS-CB, respectively). Also, PEG-NS-CB demonstrated higher stability, in which its profile of drug release, cytotoxicity, and LE% did not change significantly three months after preparation compared to those at the production time. In addition, the in vivo results demonstrated that PEG-NS-CB caused higher therapeutic (the number of alive mice: 12, 15, and 17 out of 20 in CB, NS-CB, and PEG-NS-CB receiver groups, respectively) and less toxicity effects (weight loss of 17, 12.5, and 10% in CB, NS-CB, and PEG-NS-CB receiver groups, respectively), compared to NS-CB and CB in breast cancer-bearing mice. Overall, the results of this study suggest that PEG-NS-CB could be a promising formulation for the treatment of breast cancer.

PEG-grafted liposomes for enhanced antibacterial and antibiotic activities: An in vivo study.

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 (MBIC50): 4.0 ± 0.18, 1.0 ± 0.04, and 0.5 ± 0.02 µg/mL for NF, Lip-NF, and PEG-Lip-NF, respectively). PEG-Lip-NF, compared to NF and Lip-NF, could also more efficiently decrease the side effects of NF through improving human MG-63 osteoblast cell viability (cell viability at 100 µM of NF: 76, 68, and 38% for PEG-Lip-NF, Lip-NF, and NF, respectively). PEG-Lip-NF, compared to control, NF, and Lip-NF groups, was more efficacious by 45, 25, and 10%, respectively, to decrease the virulence of MSSA bacteremia through inhibiting the weight loss of the infected mice. Also, PEG-Lip-NF and Lip-NF, compared to control and NF groups, caused a considerable decrease in the mortality rate in a murine model of bacteremia (number of dead mice: 0, 0, 2, and 8 out of 15 for PEG-Lip-NF, Lip-NF, NF, and control groups, respectively). Overall, the results of this study demonstrated that the loading of NF into PEG-Lip is a promising strategy to decrease the side effects of NF with improved antibacterial effects for the treatment of MSSA biofilm-associated infections.

Enhancing the efficacy of albendazole for liver cancer treatment using mesoporous silica nanoparticles: an in vitro study.

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 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, both ABZ and ABZ-loaded MCM-41 NPs could restrain the cell migration by 12 %. 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. See also the Graphical Abstract(Fig. 1).

Anthelmintics for drug repurposing: Opportunities and 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.

GLP-1 peptide analogs for targeting pancreatic beta cells.

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.

In Vitro Assessment of Magnetic Liposomal Paclitaxel Nanoparticles as a Potential Carrier for the Treatment of Ovarian Cancer.

Purpose: This study aimed to evaluate the role of magnetic liposome nanoparticles (ML NPs) as a carrier for paclitaxel (PTX) for the treatment of ovarian cancer in vitro. Methods: Magnetic NPs (MNPs) were synthesized by chemical co-precipitation method. The resulting NPs were characterized in terms of size, size distribution, zeta potential, drug encapsulation efficiency (EE), drug release pattern, and cytotoxicity effects. Results: The size and zeta potential of PTX-PEG-L and PTX-PEG-ML NPs were determined to be 296, 198 nm; -20, and -19 mV, respectively. Also, their drug encapsulation efficiencies were determined to be 97% and 96%, respectively. It was found that PTX-PEG-ML NPs, compared to PTX-PEG-L NPs, caused a reduction (11%) in the rate of drug release. The cytotoxicity of the drug-loaded NPs was assessed using 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay against human ovarian epithelial cancer (A2780CP) cells, and the results demonstrated that PTX-PEG-ML NPs caused higher cytotoxicity (by 14%) compared to PTX-PEG-L NPs (IC50: 1.88 ± 0.09 and 2.142 ± 0.1 µM, respectively). Conclusion: Overall, the results of this study suggest that PTX-PEG-ML NPs could be considered as a therapeutic candidate for the treatment of ovarian cancer.

Serum levels of CC chemokine ligands in cutaneous leishmaniasis patients.

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.

Mesoporous silica nanoparticles: synthesis methods and their therapeutic use-recent advances.

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.

Enhanced Efficacy of PEGylated Liposomal Cisplatin: In Vitro and In Vivo Evaluation.

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 (221-274 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 ± 0.5 and 2.3 ± 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.

Comparative analysis between four model nanoformulations of amphotericin B-chitosan, amphotericin B-dendrimer, betulinic acid-chitosan and betulinic acid-dendrimer for treatment of Leishmania major: real-time PCR assay plus.

BACKGROUND: Amphotericin B (Amp) and Betulinic acid (BA) as antileishmanial agents have negligible water solubility and high toxicity. To solve these problems, for the first time, chitosan nanoparticles and Anionic Linear Globular Dendrimer (D) were synthesized for the treatment of Leishmania major (L. major). METHOD: Chitosan and dendrimer nanoparticles were synthesized, and Amp and BA were loaded into the nanoparticles. The particles were then characterized using various methods and their efficacy was evaluated in vitro and in vivo environments (parasite burden was confirmed using pathological studies and real-time PCR methods). RESULT: The results of docking showed that Amp and BA can be loaded into chitosan and dendrimer nanoparticles. The results of physically drug loading efficiency for AK (Amphotericin B-chitosan), BK (Betulinic acid-chitosan), AD (Amphotericin B-Dendrimer) and BD (Betulinic acid- Dendrimer) were 90, 93, 84 and 96 percent, respectively. The characterization results indicated that the drugs were loaded into nanoparticles physically. Moreover, the increased solubility rate for AD=478, BD=790, AK=80 and BK=300 folds. Furthermore, the results of the drug delivery system showed the slow controlled drug release pattern with cellular uptake of more than 90%. The treatment results showed a 100 percent decrease of toxicity for the all nanodrugs was observed in vivo and in vitro environments. Moreover, AK10 and BK20 mg/kg reduced parasite burden by 83 percent (P<0.001), while AD50 and BD40 mg/kg reduced it to a lesser extent compared to glucantime. CONCLUSION: All the synthesized nanodrugs were completely succeeded by 100% to recovery the L. major induced pathological effects in the infected footpad. Also, the results of present study were confirmed with real-time PCR and the results showed that AK and BK were succeeded in a large extent to the treatment of L. major infection (P<0.001), therefore AK and BK could be considered as proper alternatives of choices drugs.

Cisplatin-Loaded Polybutylcyanoacrylate Nanoparticles with Improved Properties as an Anticancer Agent.

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' 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&E) staining were used. The results showed that the size and the drug loading efficiency of the synthesized spherical NPs were 355­386 nm and 14­19%, 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.

Evaluation of Cisplatin Efficacy on HepG2 and E. coli Cells under Acidic Conditions

Background: Cisplatin (Cispt) is a common anticancer drug for the treatment of several malignancies, including hepatocarcinoma. However, this drug suffers from instability in aqueous solutions. The study aimed to evaluate cisplatin efficacy on HepG2 and E. coli cells under an acidic condition. Methods: Acidic Cispt was prepared via incubation in acidic condition (pH=2) for a month duration. The chemical structure of the acidic Cispt was evaluated by using Fourier Transform Infrared Spectroscopy (FTIR) method. The cytotoxicity of the standard and acidic Cispt were then determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and minimum inhibitory concentration (MIC) assays on HepG2 and E. coli cells, respectively. Results: After preparing of acidic Cispt, its chemical structure was determined by FTIR method. In addition, cytotoxicity effects of Cispt in the standard and acidic forms were calculated 58 ± 2.9 and 65 ± 3.25 µM, respectively. MIC results also confirmed the results of MTT assay. MIC results for the standard and acidic Cispt were estimated 9.5 ± 0.47 and 9.8 ± 0.49 µM, respectively. Conclusion: Preparing Cispt in acidic condition not only did not degrade the drug, but also kept the potency of the drug approximately equal to parent drug. Regarding the instability issues of Cispt, keeping Cispt in acidic condition could be a promising approach to preserve its efficacy.