Injectable camptothecin conjugated hydrogels with simultaneous drug release and degradation

RSC Advances ◽  
2016 ◽  
Vol 6 (97) ◽  
pp. 94661-94668 ◽  
Author(s):  
Lilong Gao ◽  
Yadong Chen ◽  
Qiaojie Luo ◽  
Ying Wang ◽  
Xiaodong Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Hepg2 Cells ◽  
Potential Candidate ◽  
Degradation Properties

Novel injectable camptothecin conjugated hydrogels with simultaneous drug release and degradation properties were prepared, which show significant cytotoxicity to HepG2 cells, and could be a potential candidate for intratumor drug delivery.

scholarly journals Formulation and Evaluation of Floating Matrix Tablets of Sacubitril and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 298-309
Author(s):  
Sudhakar Pathak ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Potential Candidate ◽  
In Vitro Drug Release ◽  
Gastric Emptying Rate ◽  
Floating Tablets

Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The purpose of this research was to develop and evaluated floating matrix tablets of sacubitril and valsartan. The floating matrix tablets of sacubitril and valsartan were prepared by direct compression method using altered concentrations of HPMC K4M, HPMC K100M, sodium alginate as polymers and sodium bicarbonate, citric acid as gas generating agent. FTIR, DSC studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the pharmacopoeias limit. Tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, buoyancy determination and kinetic analysis of dissolution data. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. Tablet showed ≤ 1min lag time, continuance of buoyancy for >12 h. The in-vitro drug release pattern of sacubitril and valsartan optimized floating tablets (F16) was fitted to different kinetic models which showed highest regression (r2 = 0.9838) for Higuchi model. The Optimized formulation (F16) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months.  Prepared floating tablets of sacubitril and valsartan may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.  

scholarly journals Zirconium-Porphyrin PCN-222: pH-responsive Controlled Anticancer Drug Oridonin

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Xin Leng ◽  
Hongliang Huang ◽  
Wenping Wang ◽  
Na Sai ◽  
Longtai You ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Hepg2 Cells ◽  
Drug Loading ◽  
Annexin V ◽  
Controlled Drug Release ◽  
Dapi Staining ◽  
High Drug ◽  
High Drug Loading

Drug delivery carriers with a high drug loading capacity and biocompatibility, especially for controlled drug release, are urgently needed due to the side effects and frequent dose in the traditional therapeutic method. Guided by nanomaterials, we have successfully synthesized zirconium-based metal−organic frameworks, Zr-TCPP (TCPP: tetrakis (4-carboxyphenyl) porphyrin), namely, PCN-222, which is synthesized by solvothermal method. And it has been designed as a drug delivery system (DDS) with a high drug loading of 38.77 wt%. In our work, PCN-222 has achieved pH-sensitive drug release and showed comprehensive SEM, TEM, PXRD, DSC, FTIR, and N2 adsorption-desorption. The low cytotoxicity and good biocompatibility of PCN-222 were certificated by the in vitro results from an MTT assay, DAPI staining, and Annexin V/PI double-staining even cultivated L02 cells and HepG2 cells for 48h. Furthermore, Oridonin, a commonly used cancer chemotherapy drug, is adsorbed into PCN-222 via the solvent diffusion technique. Based on an analysis of the Oridonin release profile, results suggest that it can last for more than 7 days in vitro. And cumulative release rate of Ori at the 7 d was about 86.29% and 63.23% in PBS (pH 5.5 and pH 7.2, respectively) at 37°C. HepG2 cells were chosen to research the cytotoxicity of PCN-222@Ori and free Oridonin. The results demonstrated that the PCN-222@Ori nanocarrier shows higher cytotoxicity in HepG2 cells compared to Oridonin.

scholarly journals Improvement of Drug-Loading Properties of Hydroxyapatite Particles Using Triethylamine as a Capping Agent: A Novel Approach

Crystals ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 703
Author(s):  
Yi Wen ◽  
Jinsheng Li ◽  
Haotian Lin ◽  
Hao Huang ◽  
Keke Song ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Pure Water ◽  
Potential Candidate ◽  
Capping Agent ◽  
Drug Release Profile ◽  
Novel Approach ◽  
Ethanol System

Particles that modify delivery characteristics are a focus of drug-loading research. Hydroxyapatite particles (HAPs) have excellent biocompatibility, shape controllability, and high adsorption, making them a potential candidate for drug-delivery carriers. However, there are still some defects in the current methods used to prepare HAPs. In order to avoid agglomeration and improve the drug-loading properties of HAPs, the present study provides a novel triethylamine (TEA)-capped coprecipitation template method to prepare HAPs at room temperature. In addition, pure water and anhydrous ethanol were used as solvents to investigate the capping effect of the small-molecule capping agent TEA during the synthesis of HAPs. The results showed that the HAPs prepared in the TEA ethanol system had a smaller particle size (150–250 nm), better dispersion and higher crystallinity. The results were significantly different from those of the conventional preparation methods without TEA. However, the hydroxyapatite crystal would agglomerate to a certain extent after being stored for a period of time, forming micro/nano-sized agglomerates of nanocrystals. FITR analysis and SEM observation showed that the capping effect of TEA promoted the formation of a smaller template and dispersed HAPs were quickly formed by dissolution and reprecipitation processes. The drug-loading experiments showed that the HAPs prepared in the TEA ethanol system had high drug-loading capacity (239.8 ± 13.4 mg·g−1) as well as an improved drug-release profile demonstrated in the drug-release experiment. The larger specific surface area associated with the smaller particle size was beneficial to the adsorption of drugs. After drying at 60 °C, TEA was evaporated from the HAPs which agglomerated into larger micron particles with more drug encapsulated. Thus, the effect of a sustained release was achieved. In the present research, a novel approach was developed by using triethylamine as the capping agent to prepare micro/nano-sized agglomerates of HAP nanocrystals with improved drug loading, which is predicted to have potential application in drug delivery.

scholarly journals Polysaccharide-Based Controlled Release Systems for Antipsychotic Therapeutics Delivery

2020 ◽  
Vol 11 (3) ◽  
pp. 3496-3505
Author(s):  
Pranati Srivastava ◽  
Pushpendra Kumar Tripathi
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Goodness Of Fit ◽  
Release Kinetics ◽  
Hot Water ◽  
Angle Of Repose ◽  
Potential Candidate ◽  
In Vivo Models

Researches in pharmaceutical fields are now focusing on biopolymer-based drug delivery systems for treatment of mild to severe diseases. Amongst all biopolymers, pectin is one of the frequently available and eco-friendly bio-polymer extracted from different fruit peels and abundantly available in nature. This study focuses to extract the pectin from two different fruits using different methods namely hot water-based extraction and cold maceration, involving two different fruit peels. Post extraction and isolation of polymer, study was performed for characterization of pectin powder by particle shape, particle size distribution, surface area angle of repose, flowability and tapped density. The obtained pectin was used for anti-psychotic drug delivery when incorporated into microspheres by solvent evaporation method. It’s surface morphology and release kinetics was analyzed using in vitro methods and in vivo models and kinetics of drug release (goodness of fit) was assessed. The result revealed that the pectin extracted from mango peel using soxhlation method showed good flow rate, minimum particle size and shape distribution, porosity etc. Moreover, it showed the better drug release data in both invitro and in-vivo analysis. The study concludes that in future the natural biopolymer like pectin stands as a potential candidate for formulation of drug release system for efficient delivery of drug

scholarly journals Design and Pharmaceutical Evaluation of a Nano-Enabled Crosslinked Multipolymeric Scaffold for Prolonged Intracranial Release of Zidovudine

2013 ◽  
Vol 16 (3) ◽  
pp. 470 ◽  
Author(s):  
Sheri-Lee Harilall ◽  
Yahya E Choonara ◽  
Girish Modi ◽  
Lomas K Tomar ◽  
Charu Tyagi ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Entrapment Efficiency ◽  
Drug Uptake ◽  
Aids Dementia Complex ◽  
Burst Release ◽  
Potential Candidate

Purpose. Nanomedicine explores and allows for the development of drug delivery devices with superior drug uptake, controlled release and fewer drug side-effects. This study explored the use of nanosystems to formulate an implantable drug delivery device capable of sustained zidovudine release over a prolonged period. Methods. Pectin and alginate nanoparticles were prepared by applying a salting out and controlled gelification approach, respectively. The nanoparticles were characterized by attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and dynamic light scattering (DLS) and were further evaluated for zidovudine (AZT) entrapment efficiency. Multipolymeric scaffolds were prepared by crosslinking carboxymethyl cellulose, polyethylene oxide and epsilon caprolactone for entrapment of zidovudine-loaded alginate nanoparticles to impart enhanced controlled release of zidovudine over the time period. Swelling and textural analysis were conducted on the scaffolds. Prepared scaffolds were treated with hydrochloric acid (HCl) to reduce the swelling of matrix in the hydrated environment thereby further controlling the drug release. Drug release studies in phosphate buffered saline (pH 7.4, 37°C) were undertaken on both zidovudine-loaded nanoparticles and native scaffolds containing alginate nanoparticles. Results. A higher AZT entrapment efficiency was observed in alginate nanoparticles. Biphasic release was observed with both nanoparticle formulations, exhibiting an initial burst release of drug within hours of exposure to PBS, followed by a constant release rate of AZT over the remaining 30 days of nanoparticle analysis. Exposure of the scaffolds to HCl served to reduce the drug release rate from the entrapped alginate nanoparticles and extended the AZT release up to 30 days. Conclusions. The crosslinked multipolymeric scaffold loaded with alginate nanoparticles and treated with 1% HCl showed the potential for prolonged delivery of zidovudine over a period of 30 days and therefore may be a potential candidate for use as an implantable device in treating Aids Dementia Complex. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

The Improvement of Paclitaxel Cytotoxicity using Nanocellulose based Nature Resources

2019 ◽  
Vol 1 (1) ◽  
pp. 7
Author(s):  
R Nahrowi ◽  
A Setiawan ◽  
Noviany Noviany ◽  
I Sukmana ◽  
S D Yuwono
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Natural Resources ◽  
Cell Viability ◽  
Cancer Cells ◽  
Drug Delivery System ◽  
Target Cell ◽  
Mitotic Cycle ◽  
Potential Sources ◽  
Local Accumulation

Paclitaxel is one of the cancer drugs that often used. These drug kills cancer cells byinhibiting mitotic cycle. The efficiency of paclitaxel is increased by the use ofnanomaterials as a carrier of paclitaxel. Nanomaterials can enhance encapsulationefficiency, improve the drug release to the target cell following nanomaterialdegradation, and improve local accumulation of drug in the cell through endocytosisreceptor. Nanomaterial that often used forencapsulation of paclitaxel is a polymerderived from natural resources such as cellulose. The advantages of cellulose as acarrier of paclitaxel are nontoxic, biodegradable, and very abundant from varioussources. One of the potential sources of cellulose for drug delivery system is cassavabaggase.Keywords: Paclitaxel, encapsulation, cell viability, nanocellulose

Acyclovir Loaded Solid Lipid Nanoparticle Based Cream: A Novel Drug Delivery System

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
EL- Assal I. A. ◽  
Retnowati .
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Antiviral Agent ◽  
Study Drug ◽  
Particle Size Analysis ◽  
Stability Study ◽  
Size Analysis ◽  
Solid Lipid ◽  
Dermal Delivery

Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

Development of Solid Lipid Nanoparticles of Lamivudine for Brain Targeting

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Rotation Speed ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Brain Penetration ◽  
Solid Lipid ◽  
Diffusion Technique

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.

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