Combine Drug Delivery of Thymoquinone-Doxorubicin by Cockle Shellderived pH-sensitive Aragonite CaCO3 Nanoparticles

2020 ◽  
Vol 10 (4) ◽  
pp. 518-533 ◽  
Author(s):  
Kehinde M. Ibiyeye ◽  
Abu B.Z. Zuki ◽  
Norshariza Nurdin ◽  
Mokrish Ajat
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Calcium Carbonate ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Ph Sensitive ◽  
Multiple Drug ◽  
Burst Release ◽  
Cockle Shell

Background: Cockleshell-derived aragonite calcium carbonate nanoparticles were prepared by the top-down approach for combine delivery of two types of drugs. Objective: The aim of this study was to synthesize and characterize thymoquinone-doxorubicin loaded cockle shell-derived aragonite calcium carbonate nanoparticle. Aragonite calcium carbonate nanoparticles encapsulating thymoquinone and doxorubicin alone were also prepared. Methods: The blank and drug-loaded nanoparticles were characterized by field emission scanning electron microscopy, transmission electron microscopy, Zeta potential, Fourier transformed infrared and X-ray diffraction. Drug delivery properties, in vitro drug release study at pH 7.4, 6 and 4.8, and effect of blank nanoparticles on MCF10A, 3T3, MDA MB231 cells were also analyzed. Results: The blank and drug-loaded nanoparticles were pleomorphic and their sizes varying from 53.65 ± 10.29 nm to 60.49 ± 11.36 nm with an overall negative charge. The entrapment efficiency of thymoquinone and doxorubicin were 41.6 and 95.8, respectively. The FTIR showed little alteration after loading thymoquinone and doxorubicin while XRD patterns revealed no changes in the crystallizations of nanoparticles after drug loading. The drug release kinetics of doxorubicin and thymoquinone from the nanoparticles showed a continuous and gradual release after an initial burst release was observed. At pH 4.8, about 100% of drug release was noticed, 70% at pH 6 while only 50% at pH 7.4. The cell viability was 80% at a concentration of 1000 ug/ml of blank nanoparticle. Conclusion: The cockle shell-derived pH sensitive aragonite calcium carbonate nanoparticle provides an effective and simple means of multiple drug delivery and function as a platform for pH controlled release of loaded therapeutic agents.

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 Optimization Studies on Compression Coated Floating-Pulsatile Drug Delivery of Bisoprolol

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Swati C. Jagdale ◽  
Nilesh A. Bari ◽  
Bhanudas S. Kuchekar ◽  
Aniruddha R. Chabukswar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Active Ingredient ◽  
Dosage Form ◽  
Release Kinetics ◽  
Lag Phase ◽  
Burst Release ◽  
Release Formulation ◽  
Pulsatile Drug Delivery ◽  
Core Tablet

The purpose of the present work was to design and optimize compression coated floating pulsatile drug delivery systems of bisoprolol. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The rapid release core tablet (RRCT) was prepared by using superdisintegrants with active ingredient. Press coating of optimized RRCT was done by polymer. A 32full factorial design was used for optimization. The amount of Polyox WSR205 and Polyox WSR N12K was selected as independent variables. Lag period, drug release, and swelling index were selected as dependent variables. Floating pulsatile release formulation (FPRT) F13 at level 0 (55 mg) for Polyox WSR205 and level +1 (65 mg) for Polyox WSR N12K showed lag time of 4 h with >90% drug release. The data were statistically analyzed using ANOVA, andP<0.05was statistically significant. Release kinetics of the optimized formulation best fitted the zero order model.In vivostudy confirms burst effect at 4 h in indicating the optimization of the dosage form.

PLGA Nanoparticles for Anti Tuberculosis Drug Delivery

2012 ◽  
Vol 584 ◽  
pp. 465-469 ◽  
Author(s):  
S. Malathi ◽  
S. Balasubramanian
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Double Emulsion ◽  
Plga Nanoparticles ◽  
Release Mechanism ◽  
Sustained Drug Release ◽  
Drug Release Kinetics ◽  
Evaporation Technique

Nanoparticles-based drug delivery systems have considerable potential for the treatment of tuberculosis (TB). A series of PLGA polymers with different molar feed ratios (P2:87/13, P3:83/17, P5:63/37, P6:76/24, P9:53/47) were synthesized by direct melt poly condensation method. The resulting biodegradable polymers were characterized by FTIR and 1H NMR spectroscopy. The preparation of the drug (Pyrazinamide (PZA)) encapsulated PLGA polymers were carried out by double emulsion – solvent evaporation technique. The drug loaded PLGA-NPs were analyzed by UV-visible spectroscopy and scanning electron microscopy. The drug loading efficiency and drug release kinetics varies in the following order: P9>P5>P6>P3>P2. Among the formulations, PP9 showed a uniform as well as sustained drug release. The drug release kinetics has been evaluated by Zero-order, First order, Higuchi and Koresmeyer- Peppas models and the release mechanism has also been investigated

scholarly journals TEMPO-Oxidized Cellulose Beads as Potential pH-Responsive Carriers for Site-Specific Drug Delivery in the Gastrointestinal Tract

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1030
Author(s):  
Fan Xie ◽  
Pieter De Wever ◽  
Pedro Fardim ◽  
Guy Van den Mooter
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Rate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Controlled Drug Delivery ◽  
Oxidized Cellulose ◽  
Ph Responsive ◽  
Renewable Materials ◽  
Degree Of Oxidation

The development of controlled drug delivery systems based on bio-renewable materials is an emerging strategy. In this work, a controlled drug delivery system based on mesoporous oxidized cellulose beads (OCBs) was successfully developed by a facile and green method. The introduction of the carboxyl groups mediated by the TEMPO(2,2,6,6-tetramethylpiperidine-1-oxyradical)/NaClO/NaClO2 system presents the pH-responsive ability to cellulose beads, which can retain the drug in beads at pH = 1.2 and release at pH = 7.0. The release rate can be controlled by simply adjusting the degree of oxidation to achieve drug release at different locations and periods. A higher degree of oxidation corresponds to a faster release rate, which is attributed to a higher degree of re-swelling and higher hydrophilicity of OCBs. The zero-order release kinetics of the model drugs from the OCBs suggested a constant drug release rate, which is conducive to maintaining blood drug concentration, reducing side effects and administration frequency. At the same time, the effects of different model drugs and different drug-loading solvents on the release behavior and the physical state of the drugs loaded in the beads were studied. In summary, the pH-responsive oxidized cellulose beads with good biocompatibility, low cost, and adjustable release rate have shown great potential in the field of controlled drug release.

scholarly journals Polymer-free corticosteroid dimer implants for controlled and sustained drug delivery

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Kyle Battiston ◽  
Ian Parrag ◽  
Matthew Statham ◽  
Dimitra Louka ◽  
Hans Fischer ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Inflammatory Responses ◽  
Release Kinetics ◽  
Drug Loading ◽  
Rabbit Model ◽  
Drug Carriers ◽  
Surface Erosion ◽  
Sustained Drug Delivery

AbstractPolymeric drug carriers are widely used for providing temporal and/or spatial control of drug delivery, with corticosteroids being one class of drugs that have benefitted from their use for the treatment of inflammatory-mediated conditions. However, these polymer-based systems often have limited drug-loading capacity, suboptimal release kinetics, and/or promote adverse inflammatory responses. This manuscript investigates and describes a strategy for achieving controlled delivery of corticosteroids, based on a discovery that low molecular weight corticosteroid dimers can be processed into drug delivery implant materials using a broad range of established fabrication methods, without the use of polymers or excipients. These implants undergo surface erosion, achieving tightly controlled and reproducible drug release kinetics in vitro. As an example, when used as ocular implants in rats, a dexamethasone dimer implant is shown to effectively inhibit inflammation induced by lipopolysaccharide. In a rabbit model, dexamethasone dimer intravitreal implants demonstrate predictable pharmacokinetics and significantly extend drug release duration and efficacy (>6 months) compared to a leading commercial polymeric dexamethasone-releasing implant.

scholarly journals Development of Long-Acting Injectable Ketamine Loaded PLGA Microparticles as a Non-opioid Analgesic

2021 ◽  
Vol 4 (1) ◽  
Author(s):  
Juma N. Daniels ◽  
Andrew Otte
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Opioid Analgesic ◽  
Aqueous Extraction ◽  
Pharmacokinetic Studies ◽  
Burst Release ◽  
Processing Conditions ◽  
Significant Difference ◽  
Long Acting

Background/Objective: Ketamine, a psychedelic, is a noncompetitive N-methyl-D-aspartate receptor antagonist that may also bind to mu opioid receptors.  Historically, it has been used as an anesthetic (KetalarÒ), although now has found uses as a novel, quick acting, antidepressant for treatment-resistant depression (SpravatorÒ) and could be used as an adjuvant to opioid analgesia providing opioid-sparing effects.  One major advantage over opioids is Ketamine does not suffer from respiratory depression and maintains patent airways during anesthesia.  Ketamine is only available as a short-acting injectable solution or a nasal spray. Our goal is to develop a long-acting injectable form in a biodegradable matrix poly(lactic-co-glycolic) acid (PLGA) that does not have a burst release and provides 5-7 days of steady-state plasma levels.  Methods: A mechanistic approach towards development of a long-acting injectable began with a solubility screen of Ketamine. Based on these results, experiments began with an oil in water emulsification with two theoretical drug loadings (25% and 40%) and two processing conditions – (1) aqueous extraction and (2) aqueous extraction, intermediate drying, and a 25% Ethanol wash.  The formulations were characterized for drug loading, drug release, and crystallinity and imaged using scanning electron microscopy (SEM).  Results: Minimal differences were noted in the release profiles between formulations. Although, a significant difference was noted between the two processing conditions, where the extra intermediate drying step and 25% ethanol wash resulted in a significant slowing of the drug release rate.  Conclusion and Implications: The difference in release kinetics is hypothesized to be due to densification of the PLGA matrix, based on the increase in surface roughness/wrinkling in the SEM images, crystallinity increase, and on their respective powder x-ray diffraction patterns.  Our preliminary results demonstrate the feasibility of a longer acting Ketamine using PLGA. Further refinement of these formulations and rodent pharmacokinetic studies will be done in future.

Synthesys and Characterization of PLA-CNC Matrix for Antidiabetic Drug Release Applications

2020 ◽  
Vol 988 ◽  
pp. 169-174
Author(s):  
Nufus Kanani ◽  
Yenny Meliana ◽  
Endarto Yudo Wardhono ◽  
Rahmayetty ◽  
Sri Agustina ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Loading ◽  
Study Drug ◽  
The Body ◽  
Raw Material ◽  
Poly Lactic Acid ◽  
Burst Release ◽  
Antidiabetic Drug

Recently, drug nanoparticles formulation using Poly Lactic Acid-Cellulose nanocrystal (PLA-CNC) have been introduced. PLA-CNC were prepared by emulsion method for antidiabetic drug delivery applications. PLA is one of polymer which potentially used as raw material of drug delivery because it has the ability to bind and carry drugs into cell target, but the hydrophilic character of PLA can cause the degradation of PLA in the body run slowly, so it is necessary combining PLA with CNC to improve its property. In this study, special attention has been given to the modification of PLA-CNC as a drug delivery matrix to obtain the optimum drug release of antidiabetic drugs. In this study drug release analysis was conducted at 35-39 °C and pH range 3 to 9 with varied of time dissolution 0 to 180 min. PLA-CNC matrixs were characterized using FTIR and SEM, its drug loading capacity, encapsulation efficiency and in vitro drug release behavior was determined by using UV spectrophotometer. It gave the initial burst release at the first hour at 37 °C pH 3.

scholarly journals On-Demand Drug Delivery Systems Using Nanofibers

Nanomaterials ◽  
2021 ◽  
Vol 11 (12) ◽  
pp. 3411
Author(s):  
Baljinder Singh ◽  
Kibeom Kim ◽  
Myoung-Hwan Park
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Target Location ◽  
Release Kinetics ◽  
Drug Loading ◽  
Delivery Systems ◽  
Therapeutic Effects ◽  
High Porosity ◽  
On Demand

On-demand drug-delivery systems using nanofibers are extensively applicable for customized drug release based on target location and timing to achieve the desired therapeutic effects. A nanofiber formulation is typically created for a certain medication and changing the drug may have a significant impact on the release kinetics from the same delivery system. Nanofibers have several distinguishing features and properties, including the ease with which they may be manufactured, the variety of materials appropriate for processing into fibers, a large surface area, and a complex pore structure. Nanofibers with effective drug-loading capabilities, controllable release, and high stability have gained the interest of researchers owing to their potential applications in on-demand drug delivery systems. Based on their composition and drug-release characteristics, we review the numerous types of nanofibers from the most recent accessible studies. Nanofibers are classified based on their mechanism of drug release, as well as their structure and content. To achieve controlled drug release, a suitable polymer, large surface-to-volume ratio, and high porosity of the nanofiber mesh are necessary. The properties of nanofibers for modified drug release are categorized here as protracted, stimulus-activated, and biphasic. Swellable or degradable polymers are commonly utilized to alter drug release. In addition to the polymer used, the process and ambient conditions can have considerable impacts on the release characteristics of the nanofibers. The formulation of nanofibers is highly complicated and depends on many variables; nevertheless, numerous options are available to accomplish the desired nanofiber drug-release characteristics.

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.

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Average Particle Size ◽  
Delivery Systems ◽  
Average Particle ◽  
Minor Importance ◽  
Routes Of Administration ◽  
Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

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