Development of long-acting rivastigmine drug-in-adhesive patch utilizing ion-pair strategy and characterization of controlled release mechanism

The aim of this research was to synthesize and characterize chitosan-calcium alginate as matrix isoniazid encapsulation to produce controlled release isoniazid drug. The microparticles were evaluated for surface morphology, functional groups, size particles, drug content and swelling index. The drug release kinetic was investigated at gastric and intestinal artificial pH. The results showed that isoniazid-calcium alginate-chitosan has majority particle diameter of 1001-1500 nm. The release mechanism of isoniazid was through combination of erosion and diffusion.

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Characterization of a Reservoir-Style Implant for Sustained Release of Tenofovir Alafenamide (TAF) for HIV Pre-Exposure Prophylaxis (PrEP)

Pharmaceutics ◽

10.3390/pharmaceutics11070315 ◽

2019 ◽

Vol 11 (7) ◽

pp. 315 ◽

Cited By ~ 25

Author(s):

Leah M. Johnson ◽

Sai Archana Krovi ◽

Linying Li ◽

Natalie Girouard ◽

Zach R. Demkovich ◽

...

Keyword(s):

Sustained Release ◽

Surface Area ◽

Release Mechanism ◽

Release Rates ◽

Tenofovir Alafenamide ◽

Long Acting ◽

Exposure Prophylaxis ◽

Membrane Controlled Release

Long-acting (LA) HIV pre-exposure prophylaxis (PrEP) offers the potential to improve adherence by lowering the burden of daily or on-demand regimens of antiretroviral (ARV) drugs. This paper details the fabrication and in vitro performance of a subcutaneous and trocar-compatible implant for the LA delivery of tenofovir alafenamide (TAF). The reservoir-style implant comprises an extruded tube of a biodegradable polymer, poly(ε-caprolactone) (PCL), filled with a formulation of TAF and castor oil excipient. Parameters that affect the daily release rates of TAF are described, including the surface area of the implant, the thickness of the PCL tube walls (between 45 and 200 µm), and the properties of the PCL (e.g., crystallinity). In vitro studies show a linear relationship between daily release rates and surface area, demonstrating a membrane-controlled release mechanism from extruded PCL tubes. Release rates of TAF from the implant are inversely proportional to the wall thickness, with release rates between approximately 0.91 and 0.15 mg/day for 45 and 200 µm, respectively. The sustained release of TAF at 0.28 ± 0.06 mg/day over the course of 180 days in vitro was achieved. Progress in the development of this implant platform addresses the need for new biomedical approaches to the LA delivery of ARV drugs.

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Hydrogel-clay Nanocomposites as Carriers for Controlled Release

Current Medicinal Chemistry ◽

10.2174/0929867325666180831151055 ◽

2020 ◽

Vol 27 (6) ◽

pp. 919-954 ◽

Cited By ~ 4

Author(s):

Raluca Ianchis ◽

Claudia Mihaela Ninciuleanu ◽

Ioana Catalina Gifu ◽

Elvira Alexandrescu ◽

Cristina Lavinia Nistor ◽

...

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Hybrid Materials ◽

Pharmaceutical Formulations ◽

Tree Of Life ◽

Present Review ◽

Clay Nanocomposites ◽

Delivery Platform ◽

Complex Hybrid

The present review aims to summarize the research efforts undertaken in the last few years in the development and testing of hydrogel-clay nanocomposites proposed as carriers for controlled release of diverse drugs. Their advantages, disadvantages and different compositions of polymers/biopolymers with diverse types of clays, as well as their interactions are discussed. Illustrative examples of studies regarding hydrogel-clay nanocomposites are detailed in order to underline the progressive researches on hydrogel-clay-drug pharmaceutical formulations able to respond to a series of demands for the most diverse applications. Brief descriptions of the different techniques used for the characterization of the obtained complex hybrid materials such as: swelling, TGA, DSC, FTIR, XRD, mechanical, SEM, TEM and biology tests, are also included. Enlightened by the presented data, we can suppose that hydrogel-clay nanocomposites will still be a challenging subject of global assiduous researches. We can dare to dream to an efficient drug delivery platform for the treatment of multiple affection concomitantly, these being undoubtedly like ”a tree of life” bearing different kinds of fruits and leaves proper for human healing.

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DEVELOPMENT AND CHARACTERIZATION OF CHITOSAN NANOPARTICLES LOADED NANOFIBER HYBRID SYSTEM FOR VAGINAL CONTROLLED RELEASE OF BENZYDAMINE

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2021.105801 ◽

2021 ◽

pp. 105801

Author(s):

Fatmanur Tuğcu-Demiröz ◽

Sinem Saar ◽

Adnan Altuğ Kara ◽

Ayşegül Yıldız ◽

Emre Tunçel ◽

...

Keyword(s):

Controlled Release ◽

Hybrid System ◽

Chitosan Nanoparticles

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Characterization of the Absorption of Theophylline From Immediate- and Controlled-Release Dosage Forms With a Numerical Approach Using theIn VitroDissolution-Permeation Process Using Caco-2 Cells

Drug Development and Industrial Pharmacy ◽

10.1080/03639040500214589 ◽

2005 ◽

Vol 31 (4-5) ◽

pp. 397-404 ◽

Cited By ~ 1

Author(s):

Nahla Noureddine ◽

Naima Zerrouk ◽

Ioannis Nicolis ◽

Patrick Allain ◽

Souad Sfar ◽

...

Keyword(s):

Controlled Release ◽

Numerical Approach ◽

Dosage Forms

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A New Approach to Developing Long-Acting Injectable Formulations of Anti-HIV Drugs: Poly(Ethylene Phosphoric Acid) Block Copolymers Increase the Efficiency of Tenofovir against HIV-1 in MT-4 Cells

International Journal of Molecular Sciences ◽

10.3390/ijms22010340 ◽

2020 ◽

Vol 22 (1) ◽

pp. 340

Author(s):

Ilya Nifant’ev ◽

Andrei Siniavin ◽

Eduard Karamov ◽

Maxim Kosarev ◽

Sergey Kovalchuk ◽

...

Keyword(s):

Controlled Release ◽

Block Copolymers ◽

Phosphoric Acid ◽

Hiv Infection ◽

Targeted Delivery ◽

Release Formulation ◽

Poly Ethylene ◽

Long Acting ◽

Hiv Drugs ◽

Anti Hiv

Despite the world’s combined efforts, human immunodeficiency virus (HIV), the causative agent of AIDS, remains one of the world’s most serious public health challenges. High genetic variability of HIV complicates the development of anti-HIV vaccine, and there is an actual clinical need for increasing the efficiency of anti-HIV drugs in terms of targeted delivery and controlled release. Tenofovir (TFV), a nucleotide-analog reverse transcriptase inhibitor, has gained wide acceptance as a drug for pre-exposure prophylaxis or treatment of HIV infection. In our study, we explored the potential of tenofovir disoproxil (TFD) adducts with block copolymers of poly(ethylene glycol) monomethyl ether and poly(ethylene phosphoric acid) (mPEG-b-PEPA) as candidates for developing a long-acting/controlled-release formulation of TFV. Two types of mPEG-b-PEPA with numbers of ethylene phosphoric acid (EPA) fragments of 13 and 49 were synthesized by catalytic ring-opening polymerization, and used for preparing four types of adducts with TFD. Antiviral activity of [mPEG-b-PEPA]TFD or tenofovir disoproxil fumarate (TDF) was evaluated using the model of experimental HIV infection in vitro (MT-4/HIV-1IIIB). Judging by the values of the selectivity index (SI), TFD exhibited an up to 14-fold higher anti-HIV activity in the form of mPEG-b-PEPA adducts, thus demonstrating significant promise for further development of long-acting/controlled-release injectable TFV formulations.

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Exenatide Microspheres for Monthly Controlled-Release Aided by Magnesium Hydroxide

Pharmaceutics ◽

10.3390/pharmaceutics13060816 ◽

2021 ◽

Vol 13 (6) ◽

pp. 816

Author(s):

Yuxuan Ge ◽

Zhenhua Hu ◽

Jili Chen ◽

Yujie Qin ◽

Fei Wu ◽

...

Keyword(s):

Controlled Release ◽

Dosage Form ◽

Continuous Phase ◽

Plga Microspheres ◽

Receptor Agonists ◽

Monkey Model ◽

The Matrix ◽

Glass Membrane ◽

The One ◽

Long Acting

GLP-1 receptor agonists are a class of diabetes medicines offering self-regulating glycemic efficacy and may best be administrated in long-acting forms. Among GLP-1 receptor agonists, exenatide is the one requiring the least dose so that controlled-release poly(d, l-lactic-co-glycolic acid) (PLGA) microspheres may best achieve this purpose. Based on this consideration, the present study extended the injection interval of exenatide microspheres from one week of the current dosage form to four weeks by simply blending Mg(OH)2 powder within the matrix of PLGA microspheres. Mg(OH)2 served as the diffusion channel creator in the earlier stage of the controlled-release period and the decelerator of the self-catalyzed degradation of PLGA (by the formed lactic and glycolic acids) in the later stage due to its pH-responsive solubility. As a result, exenatide gradually diffused from the microspheres through Mg(OH)2-created diffusion channels before degradation of the PLGA matrix, followed by a mild release due to Mg(OH)2-buffered degradation of the polymer skeleton. In addition, an extruding–settling process comprising squeezing the PLGA solution through a porous glass membrane and sedimentation-aided solidification of the PLGA droplets was used to prepare the microspheres to ensure narrow size distribution and 95% encapsulation efficiency in an aqueous continuous phase. A pharmacokinetic study using rhesus monkey model confirmed the above formulation design by showing a steady blood concentration profile of exenatide with reduced CMAX and dosage form index. Mg·(OH)2

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