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Daru : Journal of Faculty of Pharmacy,... Dec 2020Liqui-Pellet is potentially an emerging next-generation oral pill, which has shown promising results with unique advantages as well as displaying potential for...
AIM
Liqui-Pellet is potentially an emerging next-generation oral pill, which has shown promising results with unique advantages as well as displaying potential for commercial feasibility. Since Liqui-Pellet technology is still in its infancy, it is important to explore the parameters that can affect its performance, particularly the drug release rate. Therefore, the aim of this study is to investigate thoroughly the effect of Avicel PH101 (carrier) and Aerosil 300 (coating material) ratio (R-value) in Liqui-Pellet.
METHODS
Key parameter for Liqui-Pellet formulation in this study was the ratio of carrier and coating material. Tests were carried out to assess the physicochemical properties of different formulations. This involved looking into particle size, robustness, flowability, solid-state and drug release profile. The morphology of Liqui-Pellet was investigated by SEM.
RESULTS
It is found that R-value does not have a major effect on the success of Liqui-Pellet production. However, R-value does seem to have an effect on Liqui-Pellet size at a certain water content level and a slight effect on the drug release rate. A decrease in Avicel PH101 concentration and an increase in Aerosil 300 concentration in Liqui-Pellet formulations can reduce Liqui-Pellet size and slightly increase drug release rate by 9% after 2 h. The data shows Liqui-Pellet is resistant to friability, able to achieve exceptional flow property and have smooth surfaces, which is critical for applying coatings technology. Such properties are ideal in terms of commercial manufacturing. The XRPD and DSC both show the reduction in formulation crystallinity, which is expected in Liqui-Pellet formulation as a result of solubility of the drug in the co-solvent used in the preparation of Liqui-Pellets.
CONCLUSION
Overall it seems that R-value can affect Liqui-Pellet drug release rate and size but not on the production success rate.
Topics: Calorimetry, Differential Scanning; Cellulose; Drug Compounding; Drug Implants; Microscopy, Electron, Scanning; Naproxen; Particle Size; Powder Diffraction; Silicon Dioxide; Solubility; X-Ray Diffraction
PubMed: 32757155
DOI: 10.1007/s40199-020-00362-9 -
Ophthalmic Research 2019Inflammation is substantially contributing to the development and worsening of diabetic retinopathy in general and diabetic macular edema (DME) in particular, which... (Review)
Review
Inflammation is substantially contributing to the development and worsening of diabetic retinopathy in general and diabetic macular edema (DME) in particular, which provides the rationale to treat DME with corticosteroids. While anti-vascular endothelial growth factor (VEGF) agents are mostly chosen as a first-line treatment, there is an important role for steroids in the treatment algorithm for DME. A slow-release bioerodible dexamethasone implant and an extended-release nonbioerodible fluocinolone acetonide insert are both approved for the treatment of DME and provide the advantage of sustained drug delivery and reduced treatment burden. Steroids bare the complications of cataract progression and increase of intraocular pressure (IOP). However, with dexamethasone implant, IOP rise is well manageable with topical treatment in almost all cases. Dexamethasone implant has been shown to be effective in the treatment of naive DME as well as in eyes nonresponding to anti-VEGF agents. In these cases, early switching to steroids may be considered and has been shown to be beneficial. Fluocinolone acetonide is reserved for severe cases of chronic DME insufficiently responsive to other available therapies. Future randomized controlled trials are needed to realize the role of steroids in the current treatment algorithm of DME.
Topics: Diabetic Retinopathy; Drug Implants; Glucocorticoids; Humans; Intravitreal Injections; Macular Edema; Visual Acuity
PubMed: 31048580
DOI: 10.1159/000499540 -
Ophthalmology Mar 2018
Topics: Anti-Inflammatory Agents; Drug Implants; Humans; Immunosuppressive Agents; Treatment Outcome; Uveitis
PubMed: 29458826
DOI: 10.1016/j.ophtha.2017.09.033 -
Acta Biomaterialia Jul 2019Increased use of implantable biomedical devices demonstrates their potential in treating a wide variety of ailments and disorders in bone trauma and orthopaedic,... (Review)
Review
Increased use of implantable biomedical devices demonstrates their potential in treating a wide variety of ailments and disorders in bone trauma and orthopaedic, reconstructive, and craniofacial applications. However, the number of cases involving implant failure or malfunction due to bacterial infection have also increased in recent years. Implanted devices can facilitate the growth of bacteria as these micro-organisms have the potential to adhere to the implant and grow and develop to form biofilms. In an effort to better understand and mitigate these occurrences, biomaterials containing antimicrobial agents that can be released or presented within the local microenvironment have become an important area of research. In this review, we discuss critical factors that regulate antimicrobial therapy to sites of bone infection, such as key biomolecular considerations and platforms for delivery, as well as current in vivo models and current advances in the field. STATEMENT OF SIGNIFICANCE: This review outlines the important factors that are taken into consideration for the development of biomaterials for local delivery of therapeutics to the site of bone infections. An overview of important criteria for development of this model (such as type of bone defect, antimicrobial therapeutic, and delivery vehicle) are provided, along with current research that utilizes these considerations. Additionally, this review highlights recent clinical trials that have utilized antimicrobial therapeutics for treatment of osteomyelitis.
Topics: Animals; Anti-Infective Agents; Bacteria; Bacterial Infections; Bacterial Physiological Phenomena; Biocompatible Materials; Biofilms; Bone Diseases, Infectious; Drug Implants; Humans
PubMed: 30654212
DOI: 10.1016/j.actbio.2019.01.015 -
Expert Opinion on Drug Delivery Nov 2014Remotely triggered drug delivery devices have recently been realized as injectable or implantable formulations that enable the patient or physician to control the timing...
Remotely triggered drug delivery devices have recently been realized as injectable or implantable formulations that enable the patient or physician to control the timing and dose of drug release over an extended period. Such devices could increase patient compliance, maximize therapeutic effectiveness and minimize side effects. They can be triggered by near-infrared (NIR) light, which can harmlessly and painlessly pass through tissue at controlled doses and exposure times. We discuss the use of NIR-triggered devices and materials, with examples. Safety issues and future prospects are also addressed.
Topics: Animals; Drug Delivery Systems; Drug Implants; Humans; Infrared Rays; Pharmaceutical Preparations; Remote Sensing Technology; Technology, Pharmaceutical
PubMed: 25008774
DOI: 10.1517/17425247.2014.930435 -
Scientific Reports Jul 2022The aim of the present study was to describe foveal eversion patterns in diabetic macular edema (DME) and to assess their relationship with the course of the disease and...
The aim of the present study was to describe foveal eversion patterns in diabetic macular edema (DME) and to assess their relationship with the course of the disease and the outcome. The study was designed as prospective, observational, with two years of follow-up. DME patients were divided in two groups, one treated by combined anti-VEGF injections and dexamethasone (DEX) implants, and the other treated by fluocinolone acetonide (FAc) implant with additional anti-VEGF retreatments if needed. Main outcome measures were foveal eversion prevalence, foveal eversion patterns, best-corrected visual acuity (BCVA), central macular thickness (CMT), structural OCT metrics, number of intravitreal injections. One hundred and forty-six eyes (146 patients; 80 males; mean age 67 ± 8 years) affected by already treated DME, with 84 eyes treated with anti-VEGF/DEX treatments (mean of 10 ± 3 injections) and 62 treated with FAc implant. Looking at the treatments administered before the inclusion into the study, 84 eyes (58%) were treated with anti-VEGF injections, whereas 62 eyes (42%) underwent a combination of anti-VEGF and corticosteroids implants. DME eyes showed statistically significant improvements of LogMAR BCVA and CMT over the 2-year follow-up. Foveal eversion was found in 83 eyes (57%), categorized as follows: Pattern 1a (16;19%); Pattern 1b (22;27%) and Pattern 2 (45;54%). BCVA improvement was detected in all the subgroups, excepting for Pattern 2, which showed also significantly worse structural OCT parameters. Pattern 1b and Pattern 2 were characterized by significantly higher prevalence of persistent DME (64% and 89% of cases, respectively). Foveal eversion patterns were correlated with progressively worse DME outcome. Foveal eversion may be associated to the loss of foveal homeostasis, with consequent poor response to intravitreal treatments and worse DME outcome.
Topics: Aged; Angiogenesis Inhibitors; Dexamethasone; Diabetes Mellitus; Diabetic Retinopathy; Drug Implants; Fovea Centralis; Glucocorticoids; Humans; Intravitreal Injections; Macular Edema; Male; Middle Aged; Prospective Studies; Retrospective Studies; Visual Acuity
PubMed: 35907954
DOI: 10.1038/s41598-022-17555-8 -
BioMed Research International 2016With the objective of improving efficacy and morbidity, device manufacturers incorporate chemicals or drugs into medical implants. Using multiple reservoirs of discrete... (Review)
Review
With the objective of improving efficacy and morbidity, device manufacturers incorporate chemicals or drugs into medical implants. Using multiple reservoirs of discrete drug doses, microchips represent a new technology capable of on-demand release of various drugs over long periods of time. Herein, we review drug delivery systems, how microchips work, recent investigations, and future applications in various fields of medicine.
Topics: Drug Delivery Systems; Drug Implants; Drug Liberation; Humans; Lab-On-A-Chip Devices; Pharmaceutical Preparations
PubMed: 27376079
DOI: 10.1155/2016/1743472 -
BioMed Research International 2018of observational studies concerning the pharmacological management of diabetic macular edema (DME). (Review)
Review
OBJECTIVES OF THE STUDY
of observational studies concerning the pharmacological management of diabetic macular edema (DME).
METHODS
A literature review was conducted using the PubMed database on 1 February 2018 to identify studies evaluating the efficacy of anti-VEGF and dexamethasone (DEX) implants for DME. Studies with more than 10 patients and follow-up of more than 6 months were selected. Analyses were carried out on the overall population and on subgroups defined according to baseline visual acuity (BVA) and the patients' naïve or non-naïve status.
RESULTS
Thirty-two studies evaluating the efficacy of anti-VEGF and 31 studies evaluating the efficacy of DEX-implants were retained, concerning 6,842 and 1,703 eyes, respectively. A mean gain of +4.7 letters for a mean of 5.8 injections (mean follow-up: 15.6 months) and +9.6 letters for a mean of 1.6 injections (10.3 months) was found in the anti-VEGF and DEX-implant studies, respectively. Final VA appears to be similar for both treatment (62 letters for anti-VEGF, 61.2 letters for DEX-implant), and BVA appears lower for DEX-implant, which may partially explain the greater visual gain. The DEX-implant studies show greater gains in VA compared to the anti-VEGF studies, especially for higher BVA. Indeed, mean gains for the subgroups of patients with BVA<50 letters, 50
60 letters are +4.3, +5.8, and +3.1 letters, respectively, in the anti-VEGF studies and +10.5, +9.3, and +8.8 letters, respectively, in the DEX-implant studies. Regarding the patient's initial status, only naïve status appears to confer the best functional response in DEX-implant studies. CONCLUSION
Observational studies investigating DEX-implant report clinically similar final VA when compared to anti-VEGF, but superior visual gains in real-life practice. This latter difference could be due to the better BVA, but also to the fact that less injections were administered in the anti-VEGF observational studies than in the interventional studies.
Topics: Dexamethasone; Drug Implants; Follow-Up Studies; Glucocorticoids; Humans; Intravitreal Injections; Macular Edema; Observational Studies as Topic; Tomography, Optical Coherence; Treatment Outcome
PubMed: 30246026
DOI: 10.1155/2018/8289253 -
Biomaterials Advances Mar 2022In the present work, nanohydroxyapatites (nHAp) doped with copper and/or zinc ions were investigated for the assessment of its antibacterial activity and...
Investigation of topography effect on antibacterial properties and biocompatibility of nanohydroxyapatites activated with zinc and copper ions: In vitro study of colloids, hydrogel scaffolds and pellets.
In the present work, nanohydroxyapatites (nHAp) doped with copper and/or zinc ions were investigated for the assessment of its antibacterial activity and biocompatibility. Three forms of material with diverse surfaces were tested: nanopowder in colloidal suspension, galactose hydrogel (3,6-Anhydro-α-l-Galacto-β-d-Galactan) scaffold and pellet. The structural and morphological properties of the obtained biomaterials were comprehensively determined by using: XRPD, FT-IR, SEM-EDS, AAS, XPS and EPR techniques. The antimicrobial active ions, mostly Cu, were successfully released from the apatite structure despite the material being suspended in the porous galactose hydrogel matrix. The colloidal solutions of nanohydroxyapatites on bacterial viability revealed moderate activity of Cu-doped materials against Escherichia coli strain and significant activity against Pseudomonas aeruginosa strain. The comparative study of bacterial attachment to the hydrogel and pellet surface indicated that hydrogels were more prone to be colonized by both tested strains. Moreover, an additive of the Cu ion modified bacterial attachment and biofilms forming on nHAp:Cu and nHAp:Cu-Zn materials. In the case of hydrogels, the biofilms were scattered while these forming on other materials were more clumped. The cytotoxicity evaluation of tested biomaterials showed biocompatible properties of both nanomaterial colloidal solutions as well as galactose hydrogel eluates toward normal mouse osteoblast cell lines (7F2) and human chondrocytes (TC28A2) and osteosarcoma cell line (U2OS). The biocompatibility of tested materials was additionally confirmed by conducting a hemolysis assay which showed full hemocompatibility of nanopowder colloidal solutions and galactose-based materials. Furthermore, unaltered red blood cell morphology was visible after a short and long time of incubation with the obtained biomaterials by using confocal laser scanning microscopy (CLSM). The comparison research provided data of 7F2, TC28 and U2OS cell attachment to the galactose hydrogel surface.
Topics: Animals; Anti-Bacterial Agents; Bacteria; Biocompatible Materials; Copper; Drug Implants; Escherichia coli; Galactose; Humans; Hydrogels; Ions; Mice; Spectroscopy, Fourier Transform Infrared; Zinc
PubMed: 35525765
DOI: 10.1016/j.msec.2021.112547 -
Drug Discovery Today Aug 2019Topical eye-drop administration and intravitreal injections are the current standard for ocular drug delivery. However, patient adherence to the drug regimen and... (Review)
Review
Topical eye-drop administration and intravitreal injections are the current standard for ocular drug delivery. However, patient adherence to the drug regimen and insufficient administration frequency are well-documented challenges to this field. In this review, we describe recent advances in intraocular implants designed to deliver therapeutics for months to years, to obviate the issues of patient adherence. We highlight recent advances in monolithic ocular implants in the literature, the commercialization pipeline, and approved for the market. We also describe design considerations based on material selection, active pharmaceutical ingredient, and implantation site.
Topics: Delayed-Action Preparations; Drug Delivery Systems; Drug Implants; Eye; Humans; Ophthalmic Solutions
PubMed: 31173915
DOI: 10.1016/j.drudis.2019.05.031