In Vitro Development of a New Sponge-Based Delivery System for Intracanal Antimicrobial Administration in Endodontic Treatment

This study aimed to evaluate the in vitro performance of collagen-based sponges as a drug delivery system for intracanal antimicrobial administration. Four groups of loaded collagen-based sponges (A, 0.3% w/v amoxicillin trihydrate: potassium clavulanate (4:1); B, 0.03% w/v chlorhexidine gluconate [CHX]; C, 0.3% w/v amoxicillin trihydrate: potassium clavulanate (4:1) and 0.03% w/v CHX; D, 1% w/v amoxicillin trihydrate: potassium clavulanate (4:1) and 0.03% w/v CHX) were designed. Release kinetics were tested in vitro on cultures in Petri dishes, and the effect on bacterial biofilms was studied ex vivo on 114 extracted human single-rooted teeth. Biofilm formation was tested by scanning electron microscopy (SEM). Collagen sponges containing amoxicillin and chlorhexidine showed a time-sustained antimicrobial effect in vitro and were also able to destroy mature biofilms ex vivo. This datum was validated by means of SEM-based study of E. faecalis and S. aureus biofilms.

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QbD-Based Development and Evaluation of Time-dependent Chronopharmaceutical Drug Delivery System of Amoxicillin Trihydrate for Management of Bacterial Infection

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2018.100311 ◽

2018 ◽

Vol 10 (03) ◽

Author(s):

Shyam Narayan Prasad ◽

Ashok Kumar Sahoo ◽

Abhijit V. Gothoskar

Keyword(s):

Drug Delivery ◽

Bacterial Infection ◽

Drug Delivery System ◽

Delivery System ◽

Bacterial Infections ◽

Release Kinetics ◽

Matrix Tablets ◽

Critical Material ◽

Amoxicillin Trihydrate

The present studies discuss about the quality by design (QbD)-based development and evaluation of chronomodulated release drug delivery system of amoxicillin trihydrate for management of bacterial infection. Initially, target product profile was defined and critical quality attributes were earmarked. Risk assessment study was performed for identifying the critical material attributes. Preformulation studies were carried out, and direct compression method was employed for the preparation of bilayer matrix tablets containing a delayed and a sustained release layer for preliminary optimization. Systematic formulation optimization was carried out using central composite design by selecting the concentration of Eudragit-L100 D55 and HPMCK4M. Mathematical modeling was performed and optimized compositions of the polymers were identified from the design space. Moreover, the prepared bilayer tablets were evaluated for various tablet properties including in vitro drug release study, release kinetics evaluation and characterized for FTIR, DSC, XRD, SEM studies, in vitro was-off test, antimicrobial assay and accelerated stability studies. In a nutshell, the present studies indicated the supremacy of designing a chronomodulated release bilayer tablet formulations of amoxicillin trihydrate for effective management of bacterial infections.

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Formulation Development, Characterization and In-vitro Evaluation of Tamoxifen Loaded Liposomes

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2020/v32i630449 ◽

2020 ◽

pp. 64-82

Author(s):

Md. Mazed Hasan ◽

Md. Hamiduzzaman ◽

Ishrat Jahan ◽

A. H. M. Nazmul Hasan ◽

Md. Asaduzzaman

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Side Effects ◽

Cancer Treatment ◽

Drug Delivery System ◽

Delivery System ◽

Ex Vivo ◽

Release Kinetics ◽

Formulation Development

Background: The study was aimed to prepare and evaluate tamoxifen loaded controlled release liposomes to reduce the side effects of tamoxifen during cancer treatment. Methods: Different tamoxifen loaded liposomes were prepared by modified ether injection (MEIM) and thin film hydration method (TFHM) under prescribed conditions. The prepared liposomes were characterized by using optical microscopy, evaluating encapsulation efficiency, in-vitro and ex-vivo diffusion studies by using dialysis membrane and chicken intestinal sac respectively. Results: The data revealed that all of the liposomes were spherical in shape and stable under three physical conditions i.e. 4, 25 and 37 ± 2°C temperatures and 60 ±5% relative humidity. Additionally most of the liposomes followed zero order and class II release kinetics. It was also observed that with the increase of phospholipids and cholesterol, entrapment efficiency of liposome vesicles increased thus giving a controlled release drug delivery system but further increase reduced this efficiency at a certain level. Conclusion: The formulated control release liposomes might be a good drug delivery system for target oriented drug delivery with minimum side effects of tamoxifen during cancer treatment.

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Human Saliva-Mediated Hydrolysis of Eugenyl-β-D-Glucoside and Fluorescein-di-β-D-Glucoside in In Vivo and In Vitro Models

Biomolecules ◽

10.3390/biom11020172 ◽

2021 ◽

Vol 11 (2) ◽

pp. 172

Author(s):

Mariusz Dziadas ◽

Adam Junka ◽

Henryk Jeleń

Keyword(s):

Oral Cavity ◽

Control Sample ◽

Rapid Test ◽

Human Saliva ◽

In Vitro Models ◽

Microbial Hydrolysis ◽

Amoxicillin Trihydrate ◽

Potassium Clavulanate

Eugenyl-β-D-glucopyranoside, also referred to as Citrusin C, is a natural glucoside found among others in cloves, basil and cinnamon plants. Eugenol in a form of free aglycone is used in perfumeries, flavourings, essential oils and in medicinal products. Synthetic Citrusin C was incubated with human saliva in several in vitro models together with substrate-specific enzyme and antibiotics (clindamycin, ciprofloxacin, amoxicillin trihydrate and potassium clavulanate). Citrusin C was detected using liquid chromatography with tandem mass spectrometry (LC-MS/MS). Citrusin C was completely degraded only when incubated with substrate-specific A. niger glucosidase E.C 3.2.1.21 (control sample) and when incubated with human saliva (tested sample). The addition of antibiotics to the above-described experimental setting, stopped Citrusin C degradation, indicating microbiologic origin of hydrolysis observed. Our results demonstrate that Citrusin C is subjected to complete degradation by salivary/oral cavity microorganisms. Extrapolation of our results allows to state that in the human oral cavity, virtually all β-D-glucosides would follow this type of hydrolysis. Additionally, a new method was developed for an in vivo rapid test of glucosidase activity in the human mouth on the tongue using fluorescein-di-β-D-glucoside as substrate. The results presented in this study serve as a proof of concept for the hypothesis that microbial hydrolysis path of β-D-glucosides begins immediately in the human mouth and releases the aglycone directly into the gastrointestinal tract.

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Formulation and evaluation of proniosome loaded sertaconazole nitrate for topical application

International Journal of Life Science Research Archive ◽

10.53771/ijlsra.2021.1.2.0060 ◽

2021 ◽

Vol 1 (2) ◽

pp. 023-037

Author(s):

Shailaja D ◽

Latha K ◽

Manasa D ◽

Shirisha A ◽

Padmavathi R ◽

...

Keyword(s):

Ex Vivo ◽

Release Kinetics ◽

Skin Irritation ◽

Water Soluble ◽

Ionic Surfactants ◽

Release Mechanism ◽

Stability Studies ◽

Zero Order Release ◽

Poorly Soluble

Proniosomal technology is a novel solution for poorly soluble drugs. Proniosomes are water-soluble carrier particles which are coated with non-ionic surfactants. Proniosomal gels were prepared by coacervation phase separation method using non-ionic surfactants, lipid carriers and cholesterol as a membrane stabilizer. FTIR compatibility studies revealed that the drug and excipients were compatible. All formulations were evaluated for pH, drug content, extrudability, spreadability, viscosity, in-vitro, ex-vivo, skin irritation and stability studies. Among formulations prepared, F80H1 has shown higher % EE (83.02) and least diffusion through dialysis membrane i.e., 17.68%. With ex-vivo studies, F80H1 formulation has shown highest skin deposition and lower flux of sertaconazole nitrate through the rat skin. F80H1 was selected as final optimized formulation. F80H1 exhibited good stability and SEM studies revealed that the vesicles were spherical in shape. The optimized formulation was found to follow zero order release kinetics and korsmeyer-peppas release mechanism. F80H1 found to be non-irritant and stable from skin irritation and stability studies.

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Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽

10.3390/nano11112920 ◽

2021 ◽

Vol 11 (11) ◽

pp. 2920

Author(s):

Ameeduzzafar Zafar ◽

Syed Sarim Imam ◽

Nabil K. Alruwaili ◽

Omar Awad Alsaidan ◽

Mohammed H. Elkomy ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Delivery ◽

Ex Vivo ◽

In Vitro Release ◽

System Optimization ◽

Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

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Voriconazole loaded nanostructured lipid carriers based topical delivery system: QbD based designing, characterization, in-vitro and ex-vivo evaluation

Journal of Drug Delivery Science and Technology ◽

10.1016/j.jddst.2019.04.026 ◽

2019 ◽

Vol 52 ◽

pp. 303-315 ◽

Cited By ~ 26

Author(s):

Tejashree Waghule ◽

Vamshi Krishna Rapalli ◽

Gautam Singhvi ◽

Prachi Manchanda ◽

Neha Hans ◽

...

Keyword(s):

Delivery System ◽

Ex Vivo ◽

Topical Delivery ◽

Nanostructured Lipid Carriers

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Denatured collagen as support for a FGF-2 delivery system: physicochemical characterizations and in vitro release kinetics and bioactivity

Biomaterials ◽

10.1016/j.biomaterials.2003.10.026 ◽

2004 ◽

Vol 25 (17) ◽

pp. 3761-3772 ◽

Cited By ~ 39

Author(s):

Marie-France Côté ◽

Gaetan Laroche ◽

Edith Gagnon ◽

Pascale Chevallier ◽

Charles J Doillon

Keyword(s):

Delivery System ◽

Release Kinetics ◽

In Vitro Release ◽

Vitro Release

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Effect of Skin Model on In Vitro Performance of an Adhesive Dermally Applied Microarray Coated with Zolmitriptan

Journal of Pharmaceutics ◽

10.1155/2018/7459124 ◽

2018 ◽

Vol 2018 ◽

pp. 1-5 ◽

Cited By ~ 1

Author(s):

Mahmoud Ameri ◽

Hayley Lewis ◽

Paul Lehman

Keyword(s):

Human Skin ◽

Ex Vivo ◽

Full Thickness ◽

Artificial Membrane ◽

Skin Model ◽

Hydrophobic Membrane ◽

Thickness Skin ◽

In Vitro Performance

Franz cell studies, utilizing different human skin and an artificial membrane, evaluating the influence of skin model on permeation of zolmitriptan coated on an array of titanium microprojections, were evaluated. Full thickness and dermatomed ex vivo human skin, as well as a synthetic hydrophobic membrane (Strat-M®), were assessed. It was found that the choice of model demonstrated different absorption kinetics for the permeation of zolmitriptan. For the synthetic membrane only 11% of the zolmitriptan coated dose permeated into the receptor media, whilst for the dermatomed skin 85% permeated into the receptor. The permeation of zolmitriptan through full thickness skin had a significantly different absorption profile and time to maximum flux in comparison to the dermatomed skin and synthetic model. On the basis of these results dermatomed skin may be a better estimate of in vivo performance of drug-coated metallic microprojections.

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