scholarly journals Thermosensitive Gels Used to Improve Microneedle-Assisted Transdermal Delivery of Naltrexone

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 933
Author(s):  
Kevin V. Tobin ◽  
Jennifer Fiegel ◽  
Nicole K. Brogden
Keyword(s):  
Drug Delivery ◽  
Aqueous Solution ◽  
Transdermal Delivery ◽  
Release Kinetics ◽  
Poloxamer 407 ◽  
Gelation Temperature ◽  
Before And After ◽  
Application Frequency

Transdermal delivery of naltrexone (NTX) can be enhanced using microneedles, although micropores generated this way can reseal by 48 h in humans, which prevents further drug delivery from a formulation. Poloxamer 407 (P407) is a thermosensitive polymer that may extend microneedle-assisted NTX delivery time by creating an in situ gel depot in the skin. We characterized gelation temperature, drug release, and permeation of P407 gels containing 7% NTX-HCl. To investigate microneedle effects on NTX-HCl permeation, porcine skin was treated with microneedles (600 or 750 μm length), creating 50 or 100 micropores. The formulations were removed from the skin at 48 h to simulate the effect of micropores resealing in vivo, when drug delivery is blunted. Gelation temperature increased slightly with addition of NTX-HCl. In vitro NTX-HCl release from P407 formulations demonstrated first order release kinetics. Microneedle treatment enhanced NTX-HCl permeation both from aqueous solution controls and P407 gels. Steady-state flux was overall lower in the P407 conditions compared to the aqueous solution, though ratios of AUCs before and after gel removal demonstrate that P407 gels provide more sustained release even after gel removal. This may be beneficial for reducing the required application frequency of microneedles for ongoing treatment.

scholarly journals Electrospun poly (L-lactic acid)/gelatin membranes loaded with doxorubicin for effective suppression of glioblastoma cell growth in vitro and in vivo

2021 ◽  
Author(s):  
Boxun Liu ◽  
Zhizhong Jin ◽  
Haiyan Chen ◽  
Lun Liang ◽  
Yao Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Lactic Acid ◽  
Release Kinetics ◽  
Drug Loading ◽  
Composite Membranes ◽  
Spectroscopic Techniques ◽  
Loading Process

Abstract Electrospun membranes are attracting interest as a drug delivery system because of their material composition flexibility and versatile drug loading. In this study, the electrospun membrane was loaded with doxorubicin (DOX) via electrostatic adsorption for long-term drug delivery. DOX loading process was optimized by varying temperature, time, drug concentration, pH, and ionic strength of solutions. The loading process did not impair the structural properties of the membrane. Next, we investigated the drug release kinetics using spectroscopic techniques. The composite membranes released 22% of the adsorbed DOX over the first 48 h, followed by a slower and sustained release over 4 weeks. The DOX release was sensitive to acidic solutions that the release rate at pH 6.0 was 1.27 times as that at pH 7.4. The DOX-loaded membranes were found to be cytotoxic to U-87 MG cells in vitro that decreased the cell viability from 82.92% to 25.49% from 24 h to 72 h of co-incubation. These membranes showed strong efficacy in suppressing tumour growth in vivo in glioblastoma-bearing mice that decreased the tumour volume by 77.33% compared to blank membrane-treated group on Day 20. In conclusion, we have developed an effective approach to load DOX within a clinically-approved poly (L-lactic acid)/gelatin membrane for local and long-term delivery of DOX for the treatment of glioblastoma.

Understanding the burst release phenomenon: toward designing effective nanoparticulate drug-delivery systems

2020 ◽  
pp. 00-00
Author(s):  
Sourav Bhattacharjee
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Mathematical Models ◽  
Drug Delivery Systems ◽  
Release Kinetics ◽  
Burst Release ◽  
Future Directions ◽  
Short Period

Burst release of encapsulated drug with release of a significant fraction of payload into release medium within a short period, both in vitro and in vivo, remains a challenge for translation. Such unpredictable and uncontrolled release is often undesirable, especially from the perspective of developing sustained-release formulations. Moreover, a brisk release of the payload upsets optimal release kinetics. This account strives toward understanding burst release noticed in nanocarriers and investigates its causes. Various mathematical models to explain such untimely release were also examined, including their strengths and weaknesses. Finally, the account revisits current techniques of limiting burst release from nanocarriers and prioritizes future directions that harbor potential of fruitful translation by reducing such occurrences.

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.

Poloxamer 407 microspheres for orotransmucosal drug delivery. Part II: In vitro/in vivo evaluation

2010 ◽  
Vol 400 (1-2) ◽  
pp. 32-36 ◽  
Author(s):  
D. Monti ◽  
S. Burgalassi ◽  
M.S. Rossato ◽  
B. Albertini ◽  
N. Passerini ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Poloxamer 407 ◽  
In Vivo Evaluation

scholarly journals Pectin-Based Nanomaterials: Synthesis, Toxicity and Applications

2021 ◽  
Vol 33 (11) ◽  
pp. 2579-2588
Author(s):  
Mandeep Kaur ◽  
Aditya Wadhwa ◽  
Vineet Kumar
Keyword(s):  
Drug Delivery ◽  
Human Body ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Biological Origin ◽  
Nanomaterials Synthesis ◽  
The Stability ◽  
Kinetics Of

Nanomaterials of biological origin are very useful for drug delivery applications. The stability, biodegradability and biocompatibility of pectin nanomaterials in the human body make them an effective drug carrier. This review focus on different aspect of synthesis, drug encapsulation, drug release and safety of pectin-based nanomaterials. The nanomaterials can be used for the delivery of different hydrophilic and hydrophobic drugs to various organs. The release kinetics of drug loaded pectin-based nanoparticles can be studied in vitro as well as in vivo. The pectin-based nanomaterials have good pharmaco-kinetics and can ensure controlled drug delivery. However, the toxicity of pectin-based nanomaterials to human body needs to be evaluated carefully before industrial scale application.

RESEALED ERYTHROCYTES: A PROMISING APPROACH TO ENHANCE EFFICACY OF ANTICANCER DRUGS

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (03) ◽  
pp. 9-20
Author(s):  
◽  
Prathibha Salve ◽  
Rajendra Doijad ◽  
Niranjan Chivate
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Anticancer Drugs ◽  
Delivery System ◽  
Release Kinetics ◽  
Drug Loading ◽  
The Body ◽  
Zero Order Release

Targeted drug delivery system is a potential drug delivery system which delivers the drug to particular organ of interest only. This improves the therapeutic efficacy of the treatment by reducing the side effects of drug which are required in case of anticancer drugs. Erythrocytes have been the most interesting carrier and have found to possess great potential in drug targeting. Resealed erythrocytes are gaining more popularity because of their ability to circulate throughout the body, biocompatibility, zero order release kinetics, reproducibility and ease of preparation. In this review, we have made an attempt to understand the process in detail to prepare resealed erythrocytes, including its mechanism, source and isolation of erythrocytes, methods of drug loading, in vivo and in vitro characterization of resealed erythrocytes, with special emphasis on applications of resealed erythrocytes for cancer treatment. With this review we can conclude that resealed erythrocyte is a promising approach to enhance efficacy of anticancer drugs.

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