A study of the impact of excipient shielding on initial drug release using UV imaging

2018 ◽  
Vol 553 (1-2) ◽  
pp. 229-237 ◽  
Author(s):  
Tze Ning Hiew ◽  
Muhammad Ismail Bin Alaudin ◽  
Siang Meng Chua ◽  
Paul Wan Sia Heng
Keyword(s):  
Drug Release ◽  
Uv Imaging ◽  
The Impact ◽  
Initial Drug

scholarly journals The Impact of Gelatin on the Pharmaceutical Characteristics of Fucoidan Microspheres with Posaconazole

Materials ◽  
2021 ◽  
Vol 14 (15) ◽  
pp. 4087
Author(s):  
Marta Szekalska ◽  
Aleksandra Citkowska ◽  
Magdalena Wróblewska ◽  
Katarzyna Winnicka
Keyword(s):  
Antifungal Activity ◽  
Drug Release ◽  
Spray Drying ◽  
Fungal Infections ◽  
Drug Loading ◽  
High Surface ◽  
Vaginal Fluid ◽  
Sustained Drug Release ◽  
Candida Spp ◽  
The Impact

Fungal infections and invasive mycoses, despite the continuous medicine progress, are an important globally therapeutic problem. Multicompartment dosage formulations (e.g., microparticles) ensure a short drug diffusion way and high surface area of drug release, which as a consequence can provide improvement of therapeutic efficiency compared to the traditional drug dosage forms. As fucoidan is promising component with wide biological activity per se, the aim of this study was to prepare fucospheres (fucoidan microparticles) and fucoidan/gelatin microparticles with posaconazole using the one-step spray-drying technique. Pharmaceutical properties of designed fucospheres and the impact of the gelatin addition on their characteristics were evaluated. An important stage of this research was in vitro evaluation of antifungal activity of developed microparticles using different Candida species. It was observed that gelatin presence in microparticles significantly improved swelling capacity and mucoadhesiveness, and provided a sustained POS release. Furthermore, it was shown that gelatin addition enhanced antifungal activity of microparticles against tested Candida spp. strains. Microparticles formulation GF6, prepared by the spray drying of 20% fucoidan, 5% gelatin and 10% Posaconazole, were characterized by optimal mucoadhesive properties, high drug loading and the most sustained drug release (after 8 h 65.34 ± 4.10% and 33.81 ± 5.58% of posaconazole was dissolved in simulated vaginal fluid pH 4.2 or 0.1 M HCl pH 1.2, respectively).

scholarly journals The Correlation between Physical Crosslinking and Water-Soluble Drug Release from Chitosan-Based Microparticles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 455
Author(s):  
Emilia Szymańska ◽  
Katarzyna Woś-Latosi ◽  
Julia Jacyna ◽  
Magdalena Dąbrowska ◽  
Joanna Potaś ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymer Matrix ◽  
Drug Loading ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Complex Nature ◽  
Prolonged Release ◽  
Scanning Calorimetry ◽  
Burst Effect ◽  
The Impact

Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min.

scholarly journals Tuneable spheroidal hydrogel particles for cell and drug encapsulation

Soft Matter ◽  
2018 ◽  
Vol 14 (27) ◽  
pp. 5622-5627 ◽  
Author(s):  
Isabel M. Bjørge ◽  
Ana M. S. Costa ◽  
A. Sofia Silva ◽  
João P. O. Vidal ◽  
J. Miguel Nóbrega ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Cell Encapsulation ◽  
Drug Encapsulation ◽  
Drug Release Kinetics ◽  
Hydrogel Particles ◽  
The Impact

Straight-forward production of spheroidal particles allows the assessment of the impact of geometry on cell encapsulation viability and drug release kinetics.

scholarly journals Comparison of Rheological, Drug Release, and Mucoadhesive Characteristics upon Storage between Hydrogels with Unmodified or Beta-Glycerophosphate-Crosslinked Chitosan

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Emilia Szymańska ◽  
Anna Czajkowska-Kośnik ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Physicochemical Characteristics ◽  
Vaginal Mucosa ◽  
Drug Release Profile ◽  
Modified Chitosan ◽  
Long Term Storage ◽  
Crosslinked Chitosan ◽  
Chitosan Hydrogels ◽  
The Impact

The physicochemical characteristics of beta-glycerophosphate-crosslinked chitosan hydrogels were investigated upon long-term storage at ambient, accelerated, and refrigerated conditions and compared to unmodified chitosan formulations. Additionally, the impact of chitosan modification on the ex vivo mucoadhesive performance in contact with porcine vaginal mucosa and on the drug release profile from hydrogels was evaluated. Viscosity and mechanical properties of formulations with unmodified chitosan decreased significantly upon storage regardless of tested conditions as a result of hydrolytic depolymerization. Introduction of ion crosslinker exerted stabilizing effect on physicochemical performance of chitosan hydrogels but only upon storage at refrigerated conditions. Beta-glycerophosphate-modified chitosan formulations preserved organoleptic, rheological behavior, and hydrogel structure up to 3-month storage at 4 ± 2°C. Viscosity variations upon storage influenced markedly mucoadhesive properties and drug release rate from hydrogels.

Formulation and Characterization of Thermoplastic Polyurethane-Based Steroid Eluting Devices

2019 ◽  
Author(s):  
Jessica Doan ◽  
Peter Phommahaxay ◽  
Sarah Olson ◽  
Matthew A. Petersen
Keyword(s):  
Drug Release ◽  
Medical Devices ◽  
Thermoplastic Polyurethane ◽  
Release Behavior ◽  
Implantable Medical Devices ◽  
Industry Standard ◽  
Rapid Characterization ◽  
The Impact ◽  
Standard Components

We describe the formulation and manufacture of thermoplastic polyurethane (TPU)-based steroid-eluting components and the development of a versatile, material-agnostic analytical method for their rapid characterization. The impact of materials, formulation, and processing on controlled release behavior was characterized and compared to current industry standard components under physiologically relevant conditions. The combination of factors modulated drug release, offering new avenues for controlling the release of steroids from implantable medical devices.

scholarly journals Monitoring of Antimicrobial Drug Chloramphenicol Release from Electrospun Nano- and Microfiber Mats using UV Imaging and Bacterial Bioreporters

Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 487 ◽  
Author(s):  
Preem ◽  
Bock ◽  
Hinnu ◽  
Putrinš ◽  
Sagor ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Bacterial Infections ◽  
High Performance ◽  
Model Systems ◽  
Local Drug Delivery ◽  
Imaging Method ◽  
Release Behavior ◽  
Buffer Solution ◽  
Uv Imaging

New strategies are continuously sought for the treatment of skin and wound infections due to increased problems with non-healing wounds. Electrospun nanofiber mats with antibacterial agents as drug delivery systems provide opportunities for the eradication of bacterial infections as well as wound healing. Antibacterial activities of such mats are directly linked with their drug release behavior. Traditional pharmacopoeial drug release testing settings are not always suitable for analyzing the release behavior of fiber mats intended for the local drug delivery. We tested and compared different drug release model systems for the previously characterized electrospun chloramphenicol (CAM)-loaded nanofiber (polycaprolactone (PCL)) and microfiber (PCL in combination with polyethylene oxide) mats with different drug release profiles. Drug release into buffer solution and hydrogel was investigated and drug concentration was determined using either high-performance liquid chromatography, ultraviolet-visible spectrophotometry, or ultraviolet (UV) imaging. The CAM release and its antibacterial effects in disc diffusion assay were assessed by bacterial bioreporters. All tested model systems enabled to study the drug release from electrospun mats. It was found that the release into buffer solution showed larger differences in the drug release rate between differently designed mats compared to the hydrogel release tests. The UV imaging method provided an insight into the interactions with an agarose hydrogel mimicking wound tissue, thus giving us information about early drug release from the mat. Bacterial bioreporters showed clear correlations between the drug release into gel and antibacterial activity of the electrospun CAM-loaded mats.

scholarly journals Novel On-Demand 3-Dimensional (3-D) Printed Tablets Using Fill Density as an Effective Release-Controlling Tool

Polymers ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 1872 ◽  
Author(s):  
Rishi Thakkar ◽  
Amit Raviraj Pillai ◽  
Jiaxiang Zhang ◽  
Yu Zhang ◽  
Vineet Kulkarni ◽  
...  
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Amorphous State ◽  
Dosage Forms ◽  
Water Soluble ◽  
Patient Specific ◽  
3 Dimensional ◽  
Fused Deposition ◽  
3D Printed ◽  
The Impact

This research demonstrates the use of fill density as an effective tool for controlling the drug release without changing the formulation composition. The merger of hot-melt extrusion (HME) with fused deposition modeling (FDM)-based 3-dimensional (3-D) printing processes over the last decade has directed pharmaceutical research towards the possibility of printing personalized medication. One key aspect of printing patient-specific dosage forms is controlling the release dynamics based on the patient’s needs. The purpose of this research was to understand the impact of fill density and interrelate it with the release of a poorly water-soluble, weakly acidic, active pharmaceutical ingredient (API) from a hydroxypropyl methylcellulose acetate succinate (HPMC-AS) matrix, both mathematically and experimentally. Amorphous solid dispersions (ASDs) of ibuprofen with three grades of AquaSolveTM HPMC-AS (HG, MG, and LG) were developed using an HME process and evaluated using solid-state characterization techniques. Differential scanning calorimetry (DSC), powder X-ray diffraction (pXRD), and polarized light microscopy (PLM) confirmed the amorphous state of the drug in both polymeric filaments and 3D printed tablets. The suitability of the manufactured filaments for FDM processes was investigated using texture analysis (TA) which showed robust mechanical properties of the developed filament compositions. Using FDM, tablets with different fill densities (20–80%) and identical dimensions were printed for each polymer. In vitro pH shift dissolution studies revealed that the fill density has a significant impact (F(11, 24) = 15,271.147, p < 0.0001) and a strong negative correlation (r > −0.99; p < 0.0001) with the release performance, where 20% infill demonstrated the fastest and most complete release, whereas 80% infill depicted a more controlled release. The results obtained from this research can be used to develop a robust formulation strategy to control the drug release from 3D printed dosage forms as a function of fill density.

scholarly journals Effects of Starch Incorporation on the Physicochemical Properties and Release Kinetics of Alginate-Based 3D Hydrogel Patches for Topical Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 719
Author(s):  
Sara Bom ◽  
Catarina Santos ◽  
Rita Barros ◽  
Ana M. Martins ◽  
Patrizia Paradiso ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Research Work ◽  
Gelation Time ◽  
Topical Delivery ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Burst Release ◽  
Critical Material ◽  
The Impact

The development of printable hydrogel inks for extrusion-based 3D printing is opening new possibilities to the production of new and/or improved pharmaceutical forms, specifically for topical application. Alginate and starch are natural polysaccharides that have been extensively exploited due to their biocompatibility, biodegradability, viscosity properties, low toxicity, and relatively low cost. This research work aimed to study the physicochemical and release kinetic effects of starch incorporation in alginate-based 3D hydrogel patches for topical delivery using a quality by design approach. The incorporation of a pregelatinized starch is also proposed as a way to improve the properties of the drug delivery system while maintaining the desired quality characteristics. Critical material attributes and process parameters were identified, and the sensitivity and adequacy of each parameter were statistically analyzed. The impact of alginate, starch, and CaCl2·2H2O amounts on relevant quality attributes was estimated crosswise. The amount of starch revealed a synergetic impact on porosity (p = 0.0021). An evident increase in the size and quantity of open pores were detected in the as printed patches as well as after crosslinking (15.6 ± 5.2 µm). In vitro drug release studies from the optimized alginate-starch 3D hydrogel patch, using the probe Rhodamine B, showed an initial high burst release, followed by a controlled release mechanism. The results obtained also showed that the viscoelastic properties, printing accuracy, gelation time, microstructure, and release rates can be modulated by varying the amount of starch added to the system. Furthermore, these results can be considered an excellent baseline for future drug release modulation strategies.

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