scholarly journals Encapsulation of Babchi Oil in Cyclodextrin-Based Nanosponges: Physicochemical Characterization, Photodegradation, and In Vitro Cytotoxicity Studies

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 169 ◽  
Author(s):  
Sunil Kumar ◽  
Pooja ◽  
Francesco Trotta ◽  
Rekha Rao
Keyword(s):  
Essential Oil ◽  
Physicochemical Characterization ◽  
In Vitro Cytotoxicity ◽  
Traditional Medicines ◽  
Molar Ratios ◽  
Cyclodextrin Nanosponges ◽  
Cytotoxicity Studies ◽  
The Fourier Transform ◽  
Photo Stability

Babchi (Psoralea corylifolia) oil is an important essential oil used in several traditional medicines to cure various disorders. This phytotherapeutic agent possesses a number of pharmacological activities including antibacterial, antifungal, antioxidant, anti-inflammatory, immunomodulatory, and antitumor factors. However, volatile nature, poor stability, and solubility of babchi oil (BO) restrict its pharmaceutical applications. Therefore, the aim of the present work was to encapsulate this oil in β-cyclodextrin nanosponges (NS) in order to overcome the above limitations. To fabricate nanosponges, β-cyclodextrin was cross-linked with diphenyl carbonate in different molar ratios viz. 1:2, 1:4, 1:6, 1:8, and 1:10. The blank nanosponges were loaded with BO using the freeze-drying method. The particle size of the BO loaded nanosponges was found to lie between 200 and 500 nm with low polydispersity index. Furthermore, the zeta potential, the Fourier transform infrared spectroscopy, X-ray diffraction, thermal analysis, and electron microscopy were carried out for characterization of BO nanosponges. Results obtained from spectral analysis ascertained the formation of inclusion complexes. Additionally, solubilisation efficiency of BO was checked in distilled water and found enhanced by 4.95 times with optimized β-cyclodextrin nanosponges. The cytotoxicity study was carried out by the MTT assay using HaCaT cell lines. A significant improvement in photo-stability of essential oil was also observed by inclusion innanosponges. Lastly, the optimized formulation was tested for antibacterial activity using Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. Therefore, encapsulation of BO in nanosponges resulted in efficacious carrier system in terms of solubility, photo-stability, and safety of this oil along with handling benefits.

scholarly journals Encapsulation of Babchi Oil in cyclodextrin-Based Nanosponges: Physicochemical Characterization, Photodegradation and In Vitro Cytotoxicity Studies

2018 ◽  
Author(s):  
Sunil Kumar ◽  
Pooja Sihag ◽  
Francesco Trotta ◽  
Rekha Rao
Keyword(s):  
Essential Oil ◽  
Physicochemical Characterization ◽  
X Ray Diffraction ◽  
Traditional Medicines ◽  
Molar Ratios ◽  
Beta Cyclodextrin ◽  
Cyclodextrin Nanosponges ◽  
Cytotoxicity Studies

Babchi (Psoralea corylifolia) oil is an important essential oil used in several traditional medicines to cure various disorders. This phytotherapeutic agent possesses number of pharmacological activities including antibacterial, antifungal, antioxidant, anti-inflammatory, immunomodulatory and antitumor. However, volatile nature, poor stability and solubility of babchi oil (BO) restrict its pharmaceutical applications. Hence, the aim of the present work was to encapsulate this oil in β-cyclodextrin nanosponges (NS) in order to overcome above limitations. To fabricate nanosponges, β-cyclodextrin was crosslinked with diphenyl carbonate in different molar ratios viz.1:2, 1:4, 1:6, 1:8 and 1:10. The blank nanosponges were loaded with babchi oil using freeze-drying method. Particle size of the babchi oil loaded nanosponges was found to lie between 200-500 nm, with low polydispersity index. Further, zeta potential, Fourier transform infrared spectroscopy, X-ray diffraction, thermal analysis and electron microscopy were carried out for characterization of babchi oil nanosponges. Results obtained from spectral analysis ascertained the formation of inclusion complexes. Additionally, solubilisation efficiency of the babchi oil was checked in distilled water and found enhanced by 4.95 times with optimized β-cyclodextrin nanosponges. The cytotoxicity study was carried out by MTT assay using HaCaT cell lines. A significant improvement in photostability of essential oil was also observed by inclusion in   nanosponges. Lastly, the optimized formulation was tested for antibacterial activity using Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Hence, encapsulation of BO in nanosponges resulted in efficacious carrier system in terms of solubility, photostability as well as safety of this oil along with handling benefits.

Studies on Orpiment (As2S3) Quantum Dots and their Self-Assemblies

2017 ◽  
Vol 70 (10) ◽  
pp. 1093 ◽  
Author(s):  
Jinzhu Wu ◽  
Yaxiu Feng ◽  
Haishu Lin ◽  
Paul C. Ho
Keyword(s):  
Quantum Dots ◽  
Dermal Fibroblast ◽  
High Surface ◽  
In Vitro Cytotoxicity ◽  
Traditional Medicines ◽  
Competitive Reactions ◽  
Cytotoxicity Studies ◽  
Poorly Soluble ◽  
Surface Ligand

The natural mineral orpiment (As2S3) has long been used in traditional medicines for various diseases, although it is poorly soluble and has resulting low bioavailability. In this study, orpiment quantum dots (QDs) belonging to rare V–VI binary QDs were first synthesised through top-down and bottom-up routes, in which a mixture of ethanolamine and triethanolamine was used as a coordinating solvent. The as-synthesised orpiment QDs have a narrow size distribution, superior solubility, strong blue photoluminescence emission, and good stability. Preliminary in vitro cytotoxicity studies show that orpiment QDs are less cytotoxic for human normal dermal fibroblast cells but more potent against murine melanoma B16 cells through induction of apoptosis. Moreover, self-assemblies of orpiment QDs were fabricated through destroying the protective surface ligand layer surrounding the inner orpiment cores by addition of an acid. The underlying driving force is probably competitive reactions between the surface amine ligand and the introduced acid, leading to the exposure of the bare inner orpiment cores with high surface energy.

The Effect of Phase Transition Temperature on Therapeutic Efficacy of Liposomal Bortezomib

2020 ◽  
Vol 20 (6) ◽  
pp. 700-708
Author(s):  
Mitra Korani ◽  
Sara Nikoofal-Sahlabadi ◽  
Amin R. Nikpoor ◽  
Solmaz Ghaffari ◽  
Hossein Attar ◽  
...  
Keyword(s):  
Side Effects ◽  
Cell Line ◽  
Therapeutic Efficacy ◽  
Drug Loading ◽  
Particle Diameter ◽  
In Vitro Cytotoxicity ◽  
Liposomal Formulations ◽  
Cytotoxicity Studies ◽  
Anti Tumor Activity

Aims: Here, three liposomal formulations of DPPC/DPPG/Chol/DSPE-mPEG2000 (F1), DPPC/DPPG/Chol (F2) and HSPC/DPPG/Chol/DSPE-mPEG2000 (F3) encapsulating BTZ were prepared and characterized in terms of their size, surface charge, drug loading, and release profile. Mannitol was used as a trapping agent to entrap the BTZ inside the liposomal core. The cytotoxicity and anti-tumor activity of formulations were investigated in vitro and in vivo in mice bearing tumor. Background: Bortezomib (BTZ) is an FDA approved proteasome inhibitor for the treatment of mantle cell lymphoma and multiple myeloma. The low solubility of BTZ has been responsible for the several side effects and low therapeutic efficacy of the drug. Encapsulating BTZ in a nano drug delivery system; helps overcome such issues. Among NDDSs, liposomes are promising diagnostic and therapeutic delivery vehicles in cancer treatment. Objective: Evaluating anti-tumor activity of bortezomib liposomal formulations. Methods: Data prompted us to design and develop three different liposomal formulations of BTZ based on Tm parameter, which determines liposomal stiffness. DPPC (Tm 41°C) and HSPC (Tm 55°C) lipids were chosen as variables associated with liposome rigidity. In vitro cytotoxicity assay was then carried out for the three designed liposomal formulations on C26 and B16F0, which are the colon and melanoma cancer mouse-cell lines, respectively. NIH 3T3 mouse embryonic fibroblast cell line was also used as a normal cell line. The therapeutic efficacy of these formulations was further assessed in mice tumor models. Result: MBTZ were successfully encapsulated into all the three liposomal formulations with a high entrapment efficacy of 60, 64, and 84% for F1, F2, and F3, respectively. The findings showed that liposomes mean particle diameter ranged from 103.4 to 146.8nm. In vitro cytotoxicity studies showed that liposomal-BTZ formulations had higher IC50 value in comparison to free BTZ. F2-liposomes with DPPC, having lower Tm of 41°C, showed much higher anti-tumor efficacy in mice models of C26 and B16F0 tumors compared to F3-HSPC liposomes with a Tm of 55°C. F2 formulation also enhanced mice survival compared with untreated groups, either in BALB/c or in C57BL/6 mice. Conclusion: Our findings indicated that F2-DPPC-liposomal formulations prepared with Tm close to body temperature seem to be effective in reducing the side effects and increasing the therapeutic efficacy of BTZ and merits further investigation.

Recent Advances in Curcumin Nanocarriers for the Treatment of Different Types of Cancer with Special Emphasis on In Vitro Cytotoxicity and Cellular Uptake Studies

2020 ◽  
Vol 10 (5) ◽  
pp. 577-590
Author(s):  
Jai B. Sharma ◽  
Shailendra Bhatt ◽  
Asmita Sharma ◽  
Manish Kumar
Keyword(s):  
Cancer Cells ◽  
Cellular Uptake ◽  
Anticancer Agents ◽  
Targeted Delivery ◽  
In Vitro Cytotoxicity ◽  
Curcumin Nanoparticles ◽  
Cytotoxicity Studies ◽  
Delivery Technique ◽  
Different Types

Background: The potential use of nanocarriers is being explored rapidly for the targeted delivery of anticancer agents. Curcumin is a natural polyphenolic compound obtained from rhizomes of turmeric, belongs to family Zingiberaceae. It possesses chemopreventive and chemotherapeutic activity with low toxicity in almost all types of cancer. The low solubility and bioavailability of curcumin make it unable to use for the clinical purpose. The necessity of an effective strategy to overcome the limitations of curcumin is responsible for the development of its nanocarriers. Objective: This study is aimed to review the role of curcumin nanocarriers for the treatment of cancer with special emphasis on cellular uptake and in vitro cytotoxicity studies. In addition to this, the effect of various ligand conjugated curcumin nanoparticles on different types of cancer was also studied. Methods: A systematic review was conducted by extensively surfing the PubMed, science direct and other portals to get the latest update on recent development in nanocarriers of curcumin. Results: The current data from recent studies showed that nanocarriers of curcumin resulted in the targeted delivery, higher efficacy, enhanced bioavailability and lower toxicity. The curcumin nanoparticles showed significant inhibitory effects on cancer cells as compared to free curcumin. Conclusion: It can be concluded that bioavailability of curcumin and its cytotoxic effect to cancer cells can be enhanced by the development of curcumin based nanocarriers and it was found to be a potential drug delivery technique for the treatment of cancer.

scholarly journals Development and physicochemical characterization of novel porous phosphate glass bone graft substitute and in vitro comparison with xenograft

2021 ◽  
Vol 32 (6) ◽  
Author(s):  
Niketa Chauhan ◽  
Nilay Lakhkar ◽  
Amol Chaudhari
Keyword(s):  
Cell Proliferation ◽  
Physicochemical Properties ◽  
Bone Graft ◽  
Phosphate Glass ◽  
Physicochemical Characterization ◽  
Bone Graft Substitute ◽  
Organic Content ◽  
In Vitro Cytotoxicity ◽  
Porous Phosphate

AbstractThe process of bone regeneration in bone grafting procedures is greatly influenced by the physicochemical properties of the bone graft substitute. In this study, porous phosphate glass (PPG) morsels were developed and their physicochemical properties such as degradation, crystallinity, organic content, surface topography, particle size and porosity were evaluated using various analytical methods. The in vitro cytotoxicity of the PPG morsels was assessed and the interaction of the PPG morsels with Dental Pulp Stem Cells (DPSCs) was studied by measuring cell proliferation and cell penetration depth. The cell-material interactions between PPG morsels and a commercially available xenograft (XG) were compared. The PPG morsels were observed to be amorphous, biocompatible and highly porous (porosity = 58.45%). From in vitro experiments, PPG morsels were observed to be non-cytotoxic and showed better cell proliferation. The internal surface of PPG was easily accessible to the cells compared to XG.

An efficient l-proline catalyzed synthesis of pyrazolo[3,4-e][1,4]thiazepine derivatives and their in vitro cytotoxicity studies

2014 ◽  
Vol 24 (2) ◽  
pp. 553-562 ◽  
Author(s):  
A. Srikanth ◽  
S. Sarveswari ◽  
V. Vijayakumar ◽  
P. Gridharan ◽  
S. Karthikeyan
Keyword(s):  
In Vitro Cytotoxicity ◽  
Cytotoxicity Studies

Intrathecal Mafosfamide: A Preclinical Pharmacology and Phase I Trial

2005 ◽  
Vol 23 (7) ◽  
pp. 1555-1563 ◽  
Author(s):  
Susan M. Blaney ◽  
Frank M. Balis ◽  
Stacey Berg ◽  
Carola A.S. Arndt ◽  
Richard Heideman ◽  
...  
Keyword(s):  
Phase I ◽  
Phase Ii ◽  
Phase I Trial ◽  
Neoplastic Meningitis ◽  
In Vitro Cytotoxicity ◽  
Pharmacokinetic Studies ◽  
Preclinical Studies ◽  
Phase Ii Trials ◽  
Cytotoxicity Studies

Purpose Preclinical studies of mafosfamide, a preactivated cyclophosphamide analog, were performed to define a tolerable and potentially active target concentration for intrathecal (IT) administration. A phase I and pharmacokinetic study of IT mafosfamide was performed to determine a dose for subsequent phase II trials. Patients and Methods In vitro cytotoxicity studies were performed in MCF-7, Molt-4, and rhabdomyosarcoma cell lines. Feasibility and pharmacokinetic studies were performed in nonhuman primates. These preclinical studies were followed by a phase I trial in patients with neoplastic meningitis. There were five dose levels ranging from 1 mg to 6.5 mg. Serial CSF samples were obtained for pharmacokinetic studies in a subset of patients with Ommaya reservoirs. Results The cytotoxic target exposure for mafosfamide was 10 μmol/L. Preclinical studies demonstrated that this concentration could be easily achieved in ventricular CSF after intraventricular dosing. In the phase I clinical trial, headache was the dose-limiting toxicity. Headache was ameliorated at 5 mg by prolonging the infusion rate to 20 minutes, but dose-limiting headache occurred at 6.5 mg dose with prolonged infusion. Ventricular CSF mafosfamide concentrations at 5 mg exceeded target cytotoxic concentrations after an intraventricular dose, but lumbar CSF concentrations 2 hours after the dose were less than 10 μmol/L. Therefore, a strategy to alternate dosing between the intralumbar and intraventricular routes was tested. Seven of 30 registrants who were assessable for response had a partial response, and six had stable disease. Conclusion The recommended phase II dose for IT mafosfamide, administered without concomitant analgesia, is 5 mg over 20 minutes.

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