scholarly journals A Correlative Model to Predict In Vivo AUC for Nanosystem Drug Delivery with Release Rate-Limited Absorption

2012 ◽  
Vol 15 (4) ◽  
pp. 583 ◽  
Author(s):  
Mohammad Barzegar-Jalali ◽  
Kaivan Mohammadi ◽  
Ghobad Mohammadi ◽  
Hadi Valizadeh ◽  
Azim Barzegar-Jalali ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Rate ◽  
Biological Action ◽  
Theoretical Justification ◽  
In Vitro Drug Release ◽  
Proposed Model ◽  
Gaining Insight

Purpose. Drug release from nanosystems at the sites of either absorption or effect biophase is a major determinant of its biological action. Thus, in vitro drug release is of paramount importance in gaining insight for the systems performance in vivo. Methods. A novel in vitro in vivo correlation, IVIVC, model denoted as double reciprocal area method was presented and applied to 19 drugs from 55 nano formulations with total 336 data, gathered from literature. Results. The proposed model correlated the in vitro with in vivo parameters with overall error of 12.4 ± 3.9%. Also the trained version of the model predicted the test formulations with overall error of 15.8 ± 3.7% indicating the suitability of the approach. A theoretical justification was provided for the model considering the unified classical release laws. Conclusion. The model does not necessitate bolus intravenous drug data and seems to be suitable for IVIVC of drugs with release rate-limited absorption. 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.

Phase Inversion Dynamics of PLGA Solutions Related to Drug Delivery

1998 ◽  
Vol 550 ◽  
Author(s):  
A.J. Mchugh ◽  
P.D. Graham ◽  
K.J. Brodbeck
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Rate ◽  
Phase Inversion ◽  
In Vitro Drug Release ◽  
Water Influx ◽  
Initial Release ◽  
Dark Ground ◽  
Initial Drug

AbstractDark ground optical microscopy, electron microscopy, and protein release rate studies have been used to quantify the effects of formulation changes on the phase inversion dynamics and in vitro drug release properties of an injectable PLGA-based drug delivery system. Gel growth rates and water influx rates are determined from plots of the square of the respective front with time. Results show that additives that increase the solution gelation rate and produce finger-like void morphologies result in higher initial release rates. Conversely, additives that slow the rate of gelation dramatically reduce the initial drug release rate and lead to a more dense sponge-like morphology.

scholarly journals Steroid Eluting Esophageal-Targeted Drug Delivery Devices for Treatment of Eosinophilic Esophagitis

Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 557
Author(s):  
Alka Prasher ◽  
Roopali Shrivastava ◽  
Denali Dahl ◽  
Preetika Sharma-Huynh ◽  
Panita Maturavongsadit ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Porcine Model ◽  
Pharmacokinetic Studies ◽  
Specific Drug ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
3D Printed

Eosinophilic esophagitis (EoE) is a chronic atopic disease that has become increasingly prevalent over the past 20 years. A first-line pharmacologic option is topical/swallowed corticosteroids, but these are adapted from asthma preparations such as fluticasone from an inhaler and yield suboptimal response rates. There are no FDA-approved medications for the treatment of EoE, and esophageal-specific drug formulations are lacking. We report the development of two novel esophageal-specific drug delivery platforms. The first is a fluticasone-eluting string that could be swallowed similar to the string test “entero-test” and used for overnight treatment, allowing for a rapid release along the entire length of esophagus. In vitro drug release studies showed a target release of 1 mg/day of fluticasone. In vivo pharmacokinetic studies were carried out after deploying the string in a porcine model, and our results showed a high local level of fluticasone in esophageal tissue persisting over 1 and 3 days, and a minimal systemic absorption in plasma. The second device is a fluticasone-eluting 3D printed ring for local and sustained release of fluticasone in the esophagus. We designed and fabricated biocompatible fluticasone-loaded rings using a top-down, Digital Light Processing (DLP) Gizmo 3D printer. We explored various strategies of drug loading into 3D printed rings, involving incorporation of drug during the print process (pre-loading) or after printing (post-loading). In vitro drug release studies of fluticasone-loaded rings (pre and post-loaded) showed that fluticasone elutes at a constant rate over a period of one month. Ex vivo pharmacokinetic studies in the porcine model also showed high tissue levels of fluticasone and both rings and strings were successfully deployed into the porcine esophagus in vivo. Given these preliminary proof-of-concept data, these devices now merit study in animal models of disease and ultimately subsequent translation to testing in humans.

Drug Release and Pharmacokinetic Evaluation of Novel Implantable Mometasone Furoate Matrices in Rabbit Maxillary Sinuses

2021 ◽  
pp. 194589242110391
Author(s):  
Changcheng You ◽  
Ling-Fang Tseng ◽  
Alexander Pappas ◽  
Danny Concagh ◽  
Yina Kuang
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Mometasone Furoate ◽  
In Vitro Drug Release ◽  
Nasal Sprays ◽  
Maxillary Osteotomy ◽  
Maxillary Sinuses

Background Intranasal corticosteroid sprays (INCSs) used to treat chronic rhinosinusitis are suboptimal due to limited penetration into the middle meatus, rapid clearance, and poor patient compliance. A bioresorbable drug matrix, developed with the XTreoTM drug delivery platform, may overcome the limitations of INCS by providing continuous dosing over several months. Objective To evaluate the in vitro drug release and in vivo pharmacokinetics of novel mometasone furoate (MF) matrices in a rabbit dorsal maxillary osteotomy model. Methods XTreoTM matrices were formulated to consistently elute MF for up to 6 months. Matrices were surgically placed bilaterally into the maxillary sinuses of New Zealand White (NZW) rabbits. Tissue and plasma MF concentrations were measured to assess the in vivo drug delivery. The in vivo and in vitro drug release kinetics of the matrices were quantified and compared to those of rabbits receiving daily Nasonex® MF nasal sprays. Results XTreoTM matrices self-expanded upon deployment to conform to the irregular geometry of the maxillary sinus cavities in the NZW rabbits. Sustained release of MF was demonstrated in vitro and in vivo for 2 MF matrices of distinct release durations and an in vitro–in vivo correlation was established. Therapeutic levels of MF in local tissues were measured throughout the intended dosing durations. In contrast to the variable peaks and troughs of daily nasal sprays, sustained dosing via a single administration of MF matrices was confirmed by quantifiable plasma MF concentrations over the intended dosing duration. Conclusion The XTreoTM MF matrices provided targeted and efficient dosing to local sinus tissues that was superior to INCS. Sustained drug release was confirmed both in vitro and in vivo. The novel XTreoTM technology may provide precisely tuned, long-lasting drug delivery to sinus tissues with a single treatment.

scholarly journals Metronidazole- and Amoxicillin-Loaded PLGA and PCL Nanofibers as Potential Drug Delivery Systems for the Treatment of Periodontitis: In Vitro and In Vivo Evaluations

Biomedicines ◽  
2021 ◽  
Vol 9 (8) ◽  
pp. 975
Author(s):  
Shahla Mirzaeei ◽  
Mahla Mansurian ◽  
Kofi Asare-Addo ◽  
Ali Nokhodchi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
High Performance ◽  
Drug Delivery Systems ◽  
Periodontal Diseases ◽  
Delivery Systems ◽  
Electrospinning Process ◽  
In Vitro Drug Release

The purpose of this study was to prepare poly (D-L) lactide-co-glycolide (PLGA) and poly ε-caprolactone (PCL) nanofibers containing metronidazole and amoxicillin using an electrospinning process as intrapocket sustained-release drug delivery systems for the treatment of periodontal diseases. Scanning electron microscopy showed that the drug containing PLGA and PCL nanofibers produced from the electrospinning process was uniform and bead-free in morphology. The obtained nanofibers had a strong structure and resisted external tension according to the tensiometry results. The cytotoxicity results indicated acceptable cell viability (>80%). Quantification by high-performance liquid chromatography showed almost complete in vitro drug release between 7 and 9 days, whereas 14 days were required for complete drug release in vivo. No significant signs of irritation or inflammatory reaction were detected after three weeks of subcutaneous implantation of nanofibers in the animal models, thus indicating suitable compatibility. The results therefore suggest that the designed nanofibers can be used as potential commercial formulations in the treatment of periodontitis as controlled-release intrapocket drug delivery systems that can increase patient compliance. This is due to their ability to reduce the frequency of administration from three times daily in a systemic manner to once weekly as local delivery.

scholarly journals In Vitro Methods for Evaluating Drug Release of Vaginal Ring Formulations—A Critical Review

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 538 ◽  
Author(s):  
Tietz ◽  
Klein
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Immediate Release ◽  
Discriminatory Power ◽  
Current Status ◽  
Predictive Capacity ◽  
In Vitro Drug Release ◽  
In Vitro Methods

The vagina is a promising site for both local and systemic drug delivery and represents an interesting administration route for compounds with poor oral bioavailability. Whereas most of the currently marketed dosage forms were designed as immediate release formulations, intravaginal rings (IVRs) offer the possibility of a controlled vaginal drug delivery over several weeks or months. For a long time, the development of IVRs was limited to steroid-releasing formulations. Recently, IVRs have witnessed a surge of new interest as promising delivery systems for microbicides. Therefore, various novel IVR designs have been introduced. To ensure that only safe and effective IVRs will be administered to patients, it is important to properly distinguish between IVRs with desired and undesired release performance. In vitro methods for evaluating drug release of IVRs that present with sufficient predictive capacity for in vivo drug release, and discriminatory power with regard to IVRs quality, are an essential tool for this purpose. The objective of the present review article is to present the current status of in vitro drug release testing of IVRs and to critically discuss current compendial and non-official in vitro drug release methods with regard to their discriminatory power and in vivo predictivity.

scholarly journals FORMULATION AND IN VIVO EVALUATION OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM OF RAMIPRIL IN WISTAR RATS

2021 ◽  
pp. 126-136
Author(s):  
NALLAPU JAYAPAL ◽  
YAMSANI VAMSHI VISHNU
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Systemic Absorption ◽  
Content Uniformity ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Pure Drug

Objective: The aim was to formulate and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of ramipril, an antihypertensive drug to improve the solubility and bioavailability. Methods: Based on solubility studies oil phase (Sefsol 218), surfactant (Acrysol EL135), and cosurfactant (Transcutol P), respectively, were selected to prepare SNEDDS. Ramipril SNEDDS optimized employing box-Behnken design through the study of factors. All formulations were evaluated for particle size, zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), drug content, and in vitro drug release. The optimized formulation was characterized for Fourier transform infrared (FTIR), scanning electron microscopy (SEM), stability studies, and pharmacokinetic study. Results: The mean particle size, PDI, ZP, EE, content uniformity, and in vitro drug release profile of optimized ramipril-loaded SNEDDS (RF14) were found to be 75.3±2.21nm, 0.126±0.05, −24.4±5.78mV, 98.74±1.97%, 99.52±1.67%, and 98.65±1.73%, respectively. FTIR studies revealed that there is no incompatibility between drug and excipients, SEM images exhibited nanoparticles to be more porous and in spherical shape. Stability studies indicated formulation was stable for 6 months. In vivo studies were conducted for optimized formulation RF14, the Tmax was found to be 0.5±0.62 and 0.5±0.95 h for the optimized and commercial formulations respectively, while Cmax was 25.16±1.73 ng/mL was significant (p<0.05) as compared to the ramipril pure drug 8.02±0.086 ng/mL. AUC0-t of the SNEDDS formulation was higher 355.49±1.76ng h/ml compared to pure drug 116.57±1.64 ng h/ml indicated higher amount of drug concentration in blood proving better systemic absorption of ramipril from SNEDDS formulation as compared to the pure drug. Conclusion: It is concluded from the results that ramipril was successfully formulated into SNEDDS with higher concentration with fast action.

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