scholarly journals Design and Characterisation of pH-Responsive Photosensitiser-Loaded Nano-Transfersomes for Enhanced Photodynamic Therapy

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 210
Author(s):  
Sooho Yeo ◽  
Il Yoon ◽  
Woo Kyoung Lee
Keyword(s):  
Photodynamic Therapy ◽  
Drug Release ◽  
Burst Release ◽  
Ph Responsive ◽  
Pheophorbide A ◽  
Sustained Drug Release ◽  
Non Invasive ◽  
Anti Cancer ◽  
Photodynamic Activity ◽  
The Mean

Photodynamic therapy (PDT) is a non-invasive and tumour-specific therapy. Photosensitizers (PSs) (essential ingredients in PDT) aggregate easily owing to their lipophilic properties. The aim of this study was to synthesise a PS (methyl pheophorbide a, MPa) and design a biocompatible lipid-based nanocarrier to improve its bioavailability and pharmacological effects. MPa-loaded nano-transfersomes were fabricated by sonication. The characteristics of synthesised PS and nano-transfersomes were assessed. The effects of PDT were evaluated by 1,3-diphenylisobenzofuran assay and by measuring photo-cytotoxicity against HeLa and A549 cell lines. The mean particle size and zeta potential for nano-transfersomes ranged from 95.84 to 267.53 nm and −19.53 to −45.08 mV, respectively. Nano-transfersomes exhibited sustained drug release for 48 h in a physiological environment (as against burst release in an acidic environment), which enables its use as a pH-responsive drug release system in PDT with enhanced photodynamic activity and reduced side effects. The formulations showed light cytotoxicity, but no dark toxicity, which meant that light irradiation resulted in anti-cancer effects. Additionally, formulations with the smallest size exhibited photodynamic activity to a larger extent than those with the highest loading capacity or free MPa. These results suggest that our MPa-loaded nano-transfersome system is a promising anti-cancer strategy for PDT.

scholarly journals Photodynamic therapy-triggered on-demand drug release from ROS-responsive core-cross-linked micelles toward synergistic anti-cancer treatment

Nano Research ◽  
2019 ◽  
Vol 12 (5) ◽  
pp. 999-1008 ◽  
Author(s):  
Yongjuan Li ◽  
Jian Hu ◽  
Xun Liu ◽  
Yong Liu ◽  
Shixian Lv ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Drug Release ◽  
Cancer Treatment ◽  
On Demand ◽  
Anti Cancer

scholarly journals Preparation and in vitro characterization of gellan based floating beads of acetohydroxamic acid for eradication of H. pylori

2007 ◽  
Vol 57 (4) ◽  
pp. 413-427 ◽  
Author(s):  
Parauvathanahalli Rajinikanth ◽  
Brahmeshwar mishra
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Diffusion Mechanism ◽  
Oral Dosage ◽  
Acetohydroxamic Acid ◽  
Burst Release ◽  
Sustained Drug Release ◽  
H Pylori

Preparation andin vitrocharacterization of gellan based floating beads of acetohydroxamic acid for eradication ofH. pyloriGellan based floating beads of acetohydroxamic acid (AHA) were prepared by the ionotropic gellation method to achieve controlled and sustained drug release for treatment ofHelicobacter pyloriinfection. The prepared beads were evaluated for diameter, surface morphology and encapsulation efficiency. Formulation parameters like concentrations of gellan, chitosan, calcium carbonate and the drug influenced thein vitrodrug release characteristics of beads. Drug and polymer interaction studies were carried out using differential scanning calorimetry. Chitosan coating increased encapsulation efficiency of the beads and reduced the initial burst release of the drug from the beads. Kinetic treatment of the drug release data revealed a matrix diffusion mechanism. Prepared floating beads showed good antimicrobial activity (in vitro H. pyloriculture) as potent urease inhibitors. In conclusion, an oral dosage form of floating gellan beads containing AHA may form a useful stomach site specific drug delivery system for the treatment ofH. pyloriinfection.

Development of Biodegradable Injectable In situ Forming Implants for Sustained Release of Lornoxicam

2018 ◽  
Vol 16 (1) ◽  
pp. 66-78 ◽  
Author(s):  
Ruby Christian ◽  
Vaishali Thakkar ◽  
Tushar Patel ◽  
Mukesh Gohel ◽  
Lalji Baldaniya ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Maximum Plasma ◽  
Sustained Drug Release ◽  
Drug Entrapment Efficiency ◽  
Ft Ir

Objective: The focus of this study was to develop in situ injectable implants of Lornoxicam which could provide sustained drug release. Methods: Biodegradable in situ injectable implants were prepared by polymer precipitation method using polylactide-co-glycolide (PLGA). An optimized formulation was obtained on the basis of drug entrapment efficiency, gelling behavior and in vitro drug release. The compatibility of the formulation ingredients were tested by Fourier transform infrared (FT-IR) spectroscopy, and differential scanning colorimetry (DSC). SEM study was performed to characterize in vivo behavior of in situ implant. Pharmacokinetic study and in vivo gelling study of the optimized formulation were performed on Sprague-Dawley rats. Stability testing of optimized formulation was also performed. Results: The drug entrapment efficiency increased and burst release decreased with an increase in the polymer concentration. Sustained drug release was obtained up to five days. SEM photomicrographs indicated uniform gel formation. Chemical interaction between the components of the formulation was not observed by FT-IR and DSC study. Pharmacokinetic studies of the optimized formulation revealed that the maximum plasma concentration (Cmax), time to achieve Cmax (Tmax) and area under plasma concentration curve (AUC) were significantly higher than the marketed intramuscular injection of lornoxicam. Stability study of optimized batch showed no change in physical and chemical characteristics. Conclusion: Lornoxicam can be successfully formulated as in situ injectable implant that provides long-term management of inflammatory disorders with improved patient compliance.

scholarly journals Chitosan inserts for periodontitis: Influence of drug loading, plasticizer and crosslinking on in vitro metronidazole release

2007 ◽  
Vol 57 (4) ◽  
pp. 469-477 ◽  
Author(s):  
Romi Barat ◽  
Anegundha Srinatha ◽  
Jayanta Pandit ◽  
Shampa Anupurba ◽  
Neelam Mittal
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Dissolution Time ◽  
Cross Linking ◽  
Burst Release ◽  
Casting Method ◽  
The Mean ◽  
Polymer Ratio

Chitosan inserts for periodontitis: Influence of drug loading, plasticizer and crosslinking onin vitrometronidazole releaseChitosan based metronidazole (MZ) inserts were fabricated by the casting method and characterized with respect to mass and thickness uniformity, metronidazole loading andin vitrometronidazole release kinetics. The fabricated inserts exhibited satisfactory physical characteristics. The mass of inserts was in the range of 5.63 ± 0.42 to 6.04 ± 0.89 mg. The thickness ranged from 0.46 ± 0.06 to 0.49 ± 0.08 mm. Metronidazole loading was in the range of 0.98 ± 0.09 to 1.07 ± 0.07 mg except for batch CM3 with MZ loading of 2.01 ± 0.08 mg. The inserts exhibited an initial burst release at the end of 24 h, irrespective of the drug to polymer ratio, plasticizer content or cross-linking. However, further drug release was sustained over the next 6 days. Cross-linking with 10% (m/m) of glutaraldehyde inhibited the burst release by ~30% and increased the mean dissolution time (MDT) from 0.67 to 8.59 days. The decrease in drug release was a result of reduced permeability of chitosan due to cross-linking.

scholarly journals Preparation and Evaluation of Intraperitoneal Long-Acting Oxaliplatin-Loaded Multi-Vesicular Liposomal Depot for Colorectal Cancer Treatment

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 736
Author(s):  
Sharif Md Abuzar ◽  
Eun Jung Park ◽  
Yeji Seo ◽  
Juseung Lee ◽  
Seung Hyuk Baik ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Lag Phase ◽  
Burst Release ◽  
Sustained Drug Release ◽  
Long Acting ◽  
High Entrapment Efficiency

Colorectal cancer with peritoneal metastasis has a poor prognosis because of inadequate responses to systemic chemotherapy. Cytoreductive surgery followed by intraperitoneal (IP) chemotherapy using oxaliplatin has attracted attention; however, the short half-life of oxaliplatin and its rapid clearance from the peritoneal cavity limit its clinical application. Here, a multivesicular liposomal (MVL) depot of oxaliplatin was prepared for IP administration, with an expected prolonged effect. After optimization, a combination of phospholipids, cholesterol, and triolein was used based on its ability to produce MVL depots of monomodal size distribution (1–20 µm; span 1.99) with high entrapment efficiency (EE) (92.16% ± 2.17%). An initial burst release followed by a long lag phase of drug release was observed for the MVL depots system in vitro. An in vivo pharmacokinetic study mimicking the early postoperative IP chemotherapy regimen in rats showed significantly improved bioavailability, and the mean residence time of oxaliplatin after IP administration revealed that slow and continuous erosion of the MVL particles yielded a sustained drug release. Thus, oxaliplatin-loaded MVL depots presented in this study have potential for use in the treatment of colorectal cancer.

scholarly journals Polymeric Inserts Containing Eudragit® L100 Nanoparticle for Improved Ocular Delivery of Azithromycin

Biomedicines ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 466
Author(s):  
Shiva Taghe ◽  
Shahla Mirzaeei ◽  
Raid G. Alany ◽  
Ali Nokhodchi
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Hydroxyethyl Cellulose ◽  
Burst Release ◽  
Ocular Delivery ◽  
Sustained Drug Release ◽  
Diffusion Technique ◽  
Drug Solution

Polymeric inserts containing azithromycin-loaded Eudragit® L100 nanoparticles were developed to sustain the drug release and enhance its ocular performance. The solvent diffusion technique was employed to prepare nanoparticles. The developed nanoparticles (NPs) were fully characterized and investigated. The solvent casting method was used to prepare azithromycin ocular inserts (azithromycin, AZM film) by adding hydroxypropyl methylcellulose (HPMC) or hydroxyethyl cellulose (HEC) solutions after the incorporation of AZM-loaded Eudragit® L100 nanoparticles into plasticized PVA (polyvinyl alcohol) solutions. The optimized nanoparticles had a particle size of 78.06 ± 2.3 nm, zeta potential around −2.45 ± 0.69 mV, polydispersity index around 0.179 ± 0.007, and entrapment efficiency 62.167 ± 0.07%. The prepared inserts exhibited an antibacterial effect on Staphylococcus aureus and Escherichia coli cultures. The inserts containing AZM-loaded nanoparticles showed a burst release during the initial hours, followed by a sustained drug release pattern. Higher cumulative corneal permeations from AZM films were observed for the optimized formulation compared to the drug solution in the ex-vivo trans-corneal study. In comparison to the AZM solution, the inserts significantly prolonged the release of AZM in rabbit eyes (121 h). The mucoadhesive inserts containing azithromycin-loaded Eudragit® L100 nanoparticles offer a promising approach for the ocular delivery of azithromycin (antibacterial and anti-inflammatory) to treat ocular infections that require a prolonged drug delivery.

The immobilization of antibiotic-loaded polymeric coatings on osteoarticular Ti implants for the prevention of bone infections

2017 ◽  
Vol 5 (11) ◽  
pp. 2337-2346 ◽  
Author(s):  
Dan Li ◽  
Pengfei Lv ◽  
Linfeng Fan ◽  
Yaoyi Huang ◽  
Fei Yang ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Time ◽  
Burst Release ◽  
Polymeric Coatings ◽  
Sustained Drug Release ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Bone Infections

Polymeric multilayers covalently fixed to Ti surfaces could offer a sustained drug release with no initial burst release and extend the drug release time.

Enzyme and pH-responsive nanovehicles for intracellular drug release and photodynamic therapy

2017 ◽  
Vol 41 (6) ◽  
pp. 2468-2478 ◽  
Author(s):  
Ting Zhang ◽  
Shiying Huang ◽  
Huiming Lin ◽  
Na An ◽  
Ruihan Tong ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Drug Release ◽  
Cancer Treatment ◽  
Potential Application ◽  
The Novel ◽  
Ph Responsive

An enzyme and pH-responsive nanocomposite was constructed for sensitive intracellular drug release and photodynamic therapy (PDT). The novel nanoplatforms provide the potential application in cancer treatment.

scholarly journals Development of Functionalized Carbon Nano-Onions Reinforced Zein Protein Hydrogel Interfaces for Controlled Drug Release

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 621 ◽  
Author(s):  
Narsimha Mamidi ◽  
Aldo González-Ortiz ◽  
Irasema Lopez Romo ◽  
Enrique V. Barrera
Keyword(s):  
Drug Release ◽  
Colloidal Stability ◽  
Controlled Drug Release ◽  
Acoustic Cavitation ◽  
Drug Transporter ◽  
Ph Responsive ◽  
Sustained Drug Release ◽  
In Vitro Degradation ◽  
Selective Delivery

In the current study, poly 4-mercaptophenyl methacrylate-carbon nano-onions (PMPMA-CNOs = f-CNOs) reinforced natural protein (zein) composites (zein/f-CNOs) are fabricated using the acoustic cavitation technique. The influence of f-CNOs inclusion on the microstructural properties, morphology, mechanical, cytocompatibility, in-vitro degradation, and swelling behavior of the hydrogels are studied. The tensile results showed that zein/f-CNOs hydrogels fabricated by the acoustic cavitation system exhibited good tensile strength (90.18 MPa), compared with the hydrogels fabricated by the traditional method and only microwave radiation method. It reveals the magnitude of physisorption and degree of colloidal stability of f-CNOs within the zein matrix under acoustic cavitation conditions. The swelling behaviors of hydrogels were also tested and improved results were noticed. The cytotoxicity of hydrogels was tested with osteoblast cells. The results showed good cell viability and cell growth. To explore the efficacy of hydrogels as drug transporters, 5-fluorouracil (5-FU) release was measured under gastric and intestinal pH environment. The results showed pH-responsive sustained drug release over 15 days of study, and pH 7.4 showed a more rapid drug release than pH 2.0 and 4.5. Nonetheless, all the results suggest that zein/f-CNOs hydrogel could be a potential pH-responsive drug transporter for a colon-selective delivery system.

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