Dexamethasone eluting 3D printed metal devices for bone injuries

2020 ◽  
Vol 11 (6) ◽  
pp. 373-386
Author(s):  
Ishwor Poudel ◽  
Manjusha Annaji ◽  
Robert D Arnold ◽  
Amal Kaddoumi ◽  
Nima Shamsaei ◽  
...  
Keyword(s):  
Chondroitin Sulfate ◽  
Slow Release ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Burst Release ◽  
Release Studies ◽  
3D Printed ◽  
Large Animals

Aim: Additively manufactured (3D printed), stainless steel implants were coated with dexamethasone using gelatin, chondroitin sulfate for use in bone graft surgeries. Materials & methods: The drug and polymers were deposited on the implants with a rough surface using a high precision air brush. The gelatin-chondroitin sulfate layers were cross-linked using glutaraldehyde. Results: The drug content uniformity was within 100 ± 5%, and the thickness of the polymer layer was 410 ± 5.2 μm. The in vitro release studies showed a biphasic pattern with an initial burst release followed by slow release up to 3 days. Conclusion: These results are very promising as the slow release implants can be further tested in vivo in large animals, such as cattle and horses to prevent the inflammatory cascade following surgeries.

FORMULATION DEVELOPMENT AND EVALUATION OF AN IN SITU OPHTHALMIC GELLING SYSTEM OF BRIMONIDINE TARTRATE AND TIMOLOL MALEATE FOR THE TREATMENT OF GLAUCOMA

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 76-78
Author(s):  
A Shirodker ◽  
◽  
S. Bhangle ◽  
R. Gude
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Formulation Development ◽  
Timolol Maleate ◽  
Release Studies ◽  
Brimonidine Tartrate ◽  
In Situ Gelling

The present study involved formulation of an in situ gelling system of brimonidine tartrate and timolol maleate for the treatment of glaucoma. Carbopol® 980 NF, xanthum gum and hydroxypropyl methylcellulose K4 M were used as polymers. The prepared in situ gelling systems were evaluated for clarity, appearance, texture analysis, pH, viscosity, rheological properties, in vitro gelation, isotonicity, drug content uniformity, in vitro release studies, microbiological evaluation, ex vivo release studies and stability testing. The results of the attenuated total reflectance spectroscopy and differential scanning calorimetry studies confirmed that there is no incompatibility between the drugs and the excipients. The formulations exhibited pseudoplastic rheology and formulation 3 showed the highest release of both the drugs from the formulation. The stability studies showed that the formulation was stable over the given period of time. Thus, it is evident that the in situ gelling system is a promising drug delivery system for the treatment of glaucoma.

Mixed Poloxamer Nanomicelles for the Anticonvulsant Lamotrigine Drug: Solubility, Micellar Characterization, and In-Vitro Release Studies

2021 ◽  
Vol 21 (11) ◽  
pp. 5723-5735
Author(s):  
Sofiya Shaikh ◽  
Hemil Patel ◽  
Debes Ray ◽  
Vinod K. Aswal ◽  
Rakesh K. Sharma
Keyword(s):  
In Vitro Release ◽  
Systematic Investigation ◽  
Burst Release ◽  
Drug Solubility ◽  
Biphasic Model ◽  
Release Studies ◽  
Stability Data ◽  
A Chain ◽  
Vitro Release

Recently the applications of Poloxamers in drug development is promising as it facilitated the drug molecule for delivering to the correct place, at the correct time and in the correct amount. Poloxamers can form nanomicelles to encapsulate hydrophobic drugs in order to increase solubility, stability and facilitate delivery at target. In this context, the solubilization of anticonvulsant lamotrigine (LMN) drug in a chain of Poloxamers containing different polyethylene oxide and polypropylene oxide noieties were examined. The results showed better solubilization of LMN in Poloxamers contain low CMTs while poor with Poloxamers having high CMTs. Systematic investigation of two mixed Poloxamer nanomicelles (P407:P403 and P407:P105) for LMN bioavailability at body temperature (37 °C) were investigated. The solubility of LMN was enhanced in mixed P407:P403 nanomicelles with the amount of P403 and reduced in mixed P407:P105 nanomicelles with the amount of P105. LMN encapsulated mixed Poloxamer nanomicelles were found spherical in shape with ~25 nm Dh sizes. The In-Vitro release profiles of mixed Poloxamer nanomicelles demonstrated the biphasic model with initial burst release and then slowly release of LMN. Better biocompatibility of LMN in the mixed P407:P403 nanomicelles was confirmed with stability data. The results of this work were proven the mixed P407:P403 nanomicelles as efficient nanocarriers for LMN.

Diadermatic Dose Forms Of Testosterone: In-Vitro Release Studies and in-Vivo Absorption In A Human Male

1989 ◽  
Vol 15 (9) ◽  
pp. 1405-1422
Author(s):  
A. Babar ◽  
R. A. Khaleque ◽  
A. J. Cutie ◽  
F. M. Plakogiannis
Keyword(s):  
In Vitro Release ◽  
Human Male ◽  
Release Studies ◽  
In Vivo Absorption ◽  
Vitro Release

Sucrose Acetate Isobutyrate as an In situ Forming Implant for Sustained Release of Local Anesthetics

2019 ◽  
Vol 16 (4) ◽  
pp. 331-340
Author(s):  
Hanmei Li ◽  
Yuling Xu ◽  
Yuna Tong ◽  
Yin Dan ◽  
Tingting Zhou ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Local Anesthetics ◽  
Subcutaneous Injection ◽  
In Vitro Release ◽  
Pharmacokinetic Analysis ◽  
Burst Release

Objective: In this study, an injectable Sucrose Acetate Isobutyrate (SAIB) drug delivery system (SADS) was designed and fabricated for the sustained release of Ropivacaine (RP) to prolong the duration of local anesthesia. Methods: By mixing SAIB, RP, and N-methyl-2-pyrrolidone, the SADS was prepared in a sol state with low viscosity before injection. After subcutaneous injection, the pre-gel solution underwent gelation in situ to form a drug-released depot. Result: The in vitro release profiles and in vivo pharmacokinetic analysis indicated that RP-SADS had suitable controlled release properties. Particularly, the RP-SADS significantly reduced the initial burst release after subcutaneous injection in rats. Conclusion: In a pharmacodynamic analysis of rats, the duration of nerve blockade was prolonged by over 3-fold for the RP-SADS formulation compared to RP solution. Additionally, RP-SADS showed good biocompatibility in vitro and in vivo. Thus, the SADS-based depot technology is a safe drug delivery strategy for the sustained release of local anesthetics with long-term analgesia effects.

Development and Characterization of Olanzapine Loaded Poly(lactide-co-glycolide) Microspheres for Depot Injection: In vitro and In vivo Release Profiles

2019 ◽  
Vol 16 (4) ◽  
pp. 375-383 ◽  
Author(s):  
Fahad Pervaiz ◽  
Mahmood Ahmad ◽  
Lihong Li ◽  
Ghulam Murtaza
Keyword(s):  
Bulk Density ◽  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Infrared Spectrometry ◽  
Burst Release ◽  
In Vivo Release ◽  
Depot Injection ◽  
Vitro Release

Purpose: The purpose of this study was to develop a new PLGA based microsphere formulation aimed to release the olanzapine for the period of one month which will result in increased compliance. Methods: Microspheres loaded with olanzapine were prepared using oil in water emulsion and solvent evaporation technique. The microspheres were characterized by surface morphology, shape, size, bulk density, encapsulation efficiency, and Fourier transform infrared spectrometry. In vitro release studies were performed in phosphate buffer at 37°C and in vivo studies were conducted on male Sprague- Dawley rats. Results: The morphological results indicated that microspheres produced were having a smooth surface, spherical shape and the size in the range from 9.71 to 19.90 μm mean diameter. Encapsulation efficiency of olanzapine loaded microspheres was in the range of 78.53 to 96.12% and was affected by changing the ratio of lactic to glycolic acid in copolymer PLGA. The properties of PLGA and other formulation parameters had a significant impact on in vitro and in vivo release of drug from microspheres. In vitro release kinetics revealed that release of drug from microspheres is by both non-Fickian diffusion and erosion of PLGA polymer. In vivo data indicated an initial burst release and then sustained release depending on properties of PLGA, microsphere size, and bulk density. Conclusion: This study indicates that microsphere formulations developed with PLGA (75:25) and PLGA (85:15) have provided a sufficient steady release of drug for at least 30 days and can be potential candidates for 30-day depot injection drug delivery of olanzapine.

scholarly journals Formulation and evaluation of chitosan films containing sparfloxacin for the treatment of periodontitis

2019 ◽  
Vol 9 (1) ◽  
pp. 38-45 ◽  
Author(s):  
Santoshi Naik ◽  
Prasiddhi Raikar ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
Antibacterial Activity ◽  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Periodontal Pocket ◽  
Content Uniformity ◽  
Burst Release ◽  
In Vitro Antibacterial Activity ◽  
Chitosan Films

In the present study an attempt has been made to formulate and evaluate a sustained release periodontal film of Sparfloxacin with biodegradable, cost effective polymer Chitosan. The objective of the study was to formulate intra-pocket periodontal films, which could be easily placed into the periodontal pocket, and thus be capable of delivering therapeutic concentrations of drug. Sparfloxacin is an antibiotic, showing wide spectrum antibacterial activity against a number of periodontal pathogens. Hence Sparfloxacin is selected as model for site specific delivery, i.e., into periodontal pocket for the treatment of periodontitis. In the present investigation Chitosan films containing Sparfloxacin were prepared by solution casting method using acetic acid. The copolymers HPMC K4M, Sodium CMC and Eudragit RL 100 in the concentrations of 10%, 20% and 30% w/w of Chitosan were added into the polymeric solution. Propylene glycol was used as plasticizer. FT-IR and UV spectroscopic methods revealed no interaction between Sparfloxacin and polymers. The drug loaded films were evaluated for their thickness, weight variation, content uniformity, tensile strength, percent elongation, percentage moisture loss, surface pH, folding endurance, in- vitro drug release studies, in - vitro antibacterial activity and stability studies. Periodontal films showed initial burst release of drug on 1st day and then the release was sustained for a period of 8 days. In – vitro antibacterial activity was carried out on staphylococcus aureus and the antibacterial activity was retained for 96 hours. In - vitro release from periodontal films was fit to kinetic models to reveal drug release kinetics. Keywords: Periodontitis, Sparfloxacin, Bio-adhesive polymers.

scholarly journals FORMULATION AND EVALUATION OF A CHITOSAN-PVA-GELLAN INSULIN IMPLANT

2017 ◽  
Vol 9 (3) ◽  
pp. 37
Author(s):  
Satish C. S.
Keyword(s):  
Diffusion Coefficient ◽  
Insulin Release ◽  
In Vitro Release ◽  
Poly Vinyl Alcohol ◽  
Content Uniformity ◽  
Release Studies ◽  
Solution Casting Method ◽  
Implant System ◽  
Vitro Release

Objective: The purpose of this study was to ascertain the applicability of degradable materials for fabrication of an insulin release system.Methods: Insulin implants were prepared by using poly (vinyl alcohol) (PVA), gellan and chitosan by solution casting method. The prepared implants were evaluated for swellability, content uniformity, potency and purity of insulin in implants, scanning electron microscopy studies, in vitro release studies, in vitro degradation studies using lysozyme, stability studies and circular dichroism spectroscopy.Results: The swelling degree of the implants was found to be in the range of 1.07-1.56. The diffusion coefficient of water through the implant was found to depend on the calcium chloride (CaCl2) concentration. The diffusion coefficient of insulin through the chitosan-PVA-gellan in the early stages was found to be in the range of 1.99´10-5 cm2/sec to 5.24´10-5 cm2/sec and at later stages in the range of 6.9´10-6 cm2/sec to 1.10´10-5 cm2/sec. The weight of the implants was 48±0.58 mg. The insulin content in the implants was 9.86±0.10 mg. The potency of insulin extracted from the implants was 27.11±0.75 U/mg or 95.12±2.61 % of the control insulin. The in vitro release studies showed that insulin was released completely in a period of 13-19 d depending on the composition of the implant. The increase in CaCl2 retarded the rate of insulin release whereas the increase in PVA content leads to the rapid release of insulin. The device was found to undergo significant weight loss due to enzyme mediated degradation.Conclusion: These studies provide validity for the potential utility of chitosan-PVA-gellan implant systems for the delivery of insulin. The studies also demonstrate that insulin maintained its integrity within the implant system. Implants showed the complete release of insulin in 19 d and the release of insulin from the implants depended on the amount of CaCl2.

scholarly journals Ondansetron Hydrochloride in Treating Patients with Cancer and Chronic Nausea Vomiting

2017 ◽  
Vol 1 (2) ◽  
pp. 01-04
Author(s):  
Hye jin
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Extended Period ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Ondansetron Hydrochloride ◽  
Backing Layer ◽  
Carbopol 934P

The objective of this study was to develop effective bioadhesive buccal bilayered tablets comprising of drug containing bioadhesive layer and drug free backing layer, expected to release the drug in unidirection for extended period of time. Tablets of ondansetron HCl were prepared by direct compression method using bioadhesive polymers like Carbopol 934P, Methocel K4M, Methocel K15M and Hydroxy propyl cellulose in different combinations and concentrations with backing layer of ethyl cellulose. Buccal tablets were evaluated by different parameters such as thickness, hardness, weight uniformity, content uniformity, swelling index, surface pH, ex vivo bioadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation, stability studies in human saliva, in vivo mucoadhesive performance studies and FTIR studies. The modified in vitro assembly was used to measure the bioadhesive strength of tablets with fresh porcine buccal mucosa as model tissue. Bioadhesion strength was increased with increase in the concentration of carbopol. The tablets were evaluated for in vitro release in pH 6.6 phosphate buffer for 8 hr in standard dissolution apparatus. In order to improve the permeation of the drug, tauroglycholate (permeation enhancer) added in the optimized formulation at 10mM concentration. In order to determine the mode of release, the data was subjected to Korsmeyer and Peppas diffusion model. The optimized formula followed non-fickian release mechanism with zero order kinetics. Carbopol 934P and HPC in the ratio of 3:1 could be used to design effective and stable buccoadhesive tablets of ondansetron HCl. The present study concludes that buccal delivery of ondansetron HCl tablets can be good way to bypass the first pass metabolism.

scholarly journals Topical Chitosan-Based Thermo-Responsive Scaffold Provides Dexketoprofen Trometamol Controlled Release for 24 h Use

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2100
Author(s):  
Luis Castillo-Henríquez ◽  
Pablo Sanabria-Espinoza ◽  
Brayan Murillo-Castillo ◽  
Gabriela Montes de Oca-Vásquez ◽  
Diego Batista-Menezes ◽  
...  
Keyword(s):  
Controlled Release ◽  
Kinetic Models ◽  
In Vitro Release ◽  
Solution Temperature ◽  
Burst Release ◽  
Release Studies ◽  
Dexketoprofen Trometamol ◽  
Ft Ir ◽  
Healing Wounds

Chronic and non-healing wounds demand personalized and more effective therapies for treating complications and improving patient compliance. Concerning that, this work aims to develop a suitable chitosan-based thermo-responsive scaffold to provide 24 h controlled release of Dexketoprofen trometamol (DKT). Three formulation prototypes were developed using chitosan (F1), 2:1 chitosan: PVA (F2), and 1:1 chitosan:gelatin (F3). Compatibility tests were done by DSC, TG, and FT-IR. SEM was employed to examine the morphology of the surface and inner layers from the scaffolds. In vitro release studies were performed at 32 °C and 38 °C, and the profiles were later adjusted to different kinetic models for the best formulation. F3 showed the most controlled release of DKT at 32 °C for 24 h (77.75 ± 2.72%) and reduced the burst release in the initial 6 h (40.18 ± 1.00%). The formulation exhibited a lower critical solution temperature (LCST) at 34.96 °C, and due to this phase transition, an increased release was observed at 38 °C (88.52 ± 2.07% at 12 h). The release profile for this formulation fits with Hixson–Crowell and Korsmeyer–Peppas kinetic models at both temperatures. Therefore, the developed scaffold for DKT delivery performs adequate controlled release, thereby; it can potentially overcome adherence issues and complications in wound healing applications.

Fig. 12 Scanning electron micrograph of D.L-PLA nanoparticles loaded with CGP 57813. (Ref. 51.) scanning force microscopy (also called atomic force microscopy), enable the visualiza-tion of nanoparticles at atmospheric pressure without gold coating [12,64]. Neverthe-less, the resolution obtained with these new tools is still lower than that with SEM. For size determination, transmission electron microscopy is not as widely used as PCS and SEM, but it is still a powerful method for determining the morphology of particles. With this technique, Fessi et al. [42] estimated the wall thickness of PLA nanocapsules. Krause et al. [18] described the highly porous structure of PLA nano-spheres prepared by the emulsion-evaporation procedure. VIII. IN VITRO RELEASE STUDIES In vitro release studies should in principle be useful for quality control as well as for the prediction of in vivo kinetics. Unfortunately, due to the very small size of the par-ticles, the release rate observed in vivo can differ greatly from the release obtained in a buffer solution. However, in vitro release studies remain very useful for quality control as well as for evaluation of the influence of process parameters on the release rate of active compounds. In vitro drug release from microdispersed systems has been exten-sively reviewed by Washington [65]. Depending on the type of polyester, drug release from nanoparticles can take place through several processes, of which the following appear to be the most important: (1) The drug may diffuse out of the carrier through the solid matrix; to allow complete release from the carriers, (the concentration of drug in the release medium should re-main infinitely low, which condition is known as sink condition); (2) The solvent may penetrate the nanoparticles and dissolve the drug, which then diffuses out into the re-lease medium. Depending on the physico-chemical characteristics of the particles, wa-ter can enter the particles through narrow pores or by hydration. Once the drug is dis-solved, the drug diffuses out of the particles. Here again, since diffusion is driving the

1998 ◽  
pp. 204-216
Keyword(s):  
Quality Control ◽  
Drug Release ◽  
Release Rate ◽  
In Vitro Release ◽  
Scanning Force Microscopy ◽  
Force Microscopy ◽  
Release Studies ◽  
Vitro Release
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