The Experts below are selected from a list of 2202 Experts worldwide ranked by ideXlab platform
Vitaliy V Khutoryanskiy - One of the best experts on this subject based on the ideXlab platform.
-
chitosan poly 2 ethyl 2 oxazoline films with ciprofloxacin for application in Vaginal Drug Delivery
Materials, 2020Co-Authors: Guzel K Abilova, Daulet B Kaldybekov, G S Irmukhametova, Diara S Kazybayeva, Zhanar A Iskakbayeva, Sarkyt E Kudaibergenov, Vitaliy V KhutoryanskiyAbstract:Chitosan (CHI) and chitosan/poly(2-ethyl-2-oxazoline) (CHI/POZ)-based films were prepared by casting from aqueous solutions of polymer blends with different compositions. Ciprofloxacin was used as a model Drug in these formulations. The weight, thickness, folding endurance and transparency of blend films were measured and characterised. All films had a uniform thickness (0.06 ± 0.01 mm) and exhibited sufficient flexibility. The surface pHs of films ranged from 3.76 ± 0.49 to 4.14 ± 0.32, which is within the pH range suitable for Vaginal applications. The cumulative release of the Drug from the films in experiments in vitro was found to be 42 ± 2% and 56 ± 1% for pure CHI and CHI/POZ (40:60) films, respectively. Drug-free chitosan/poly(2-ethyl-2-oxazoline) films showed weak antimicrobial activity against Escherichia coli. Drug-loaded CHI and CHI/POZ films showed good antimicrobial properties against both Gram-positive Staphylococcus aureus and Gram-negative bacteria Escherichia coli. Mucoadhesive properties of these films with respect to freshly excised sheep Vaginal mucosa were evaluated using a tensile method. It was established that all films were mucoadhesive, but an increase in POZ content in the blend resulted in a gradual reduction of their ability to stick to Vaginal mucosa. These films could potentially find applications in Vaginal Drug Delivery.
-
advances in mucoadhesion and mucoadhesive polymers
Macromolecular Bioscience, 2011Co-Authors: Vitaliy V KhutoryanskiyAbstract:Mucoadhesion is the ability of materials to adhere to mucosal membranes in the human body and provide a temporary retention. This property has been widely used to develop polymeric dosage forms for buccal, oral, nasal, ocular and Vaginal Drug Delivery. Excellent mucoadhesive properties are typical for hydrophilic polymers possessing charged groups and/or non-ionic functional groups capable of forming hydrogen bonds with mucosal surfaces. This feature article considers recent advances in the study of mucoadhesion and mucoadhesive polymers. It provides an overview on the structure of mucosal membranes, properties of mucus gels and the nature of mucoadhesion. It describes the most common methods to evaluate mucoadhesive properties of various dosage forms and discusses the main classes of mucoadhesives.
Patrick F Kiser - One of the best experts on this subject based on the ideXlab platform.
-
controlling the hydration rate of a hydrophilic matrix in the core of an intraVaginal ring determines antiretroviral release
Journal of Controlled Release, 2016Co-Authors: Justin T. Clark, Ryan S Teller, David C Malaspina, Rachna Rastogi, Igal Szleifer, Patrick F KiserAbstract:IntraVaginal ring technology is generally limited to releasing low molecular weight species that can diffuse through the ring elastomer. To increase the diversity of Drugs that can be delivered from intraVaginal rings, we designed an IVR that contains a Drug matrix encapsulated in the core of the IVR whereby the mechanism of Drug release is uncoupled from the interaction of the Drug with the ring elastomer. We call the device a flux controlled pump, and it is comprised of compressed pellets of a mixture of Drug and hydroxypropyl cellulose within the hollow core of the ring. The pump orifice size and chemistry of the polymer pellets control the rate of hydration and diffusion of the Drug-containing hydroxypropyl cellulose gel from the device. A mechanistic model describing the hydration and diffusion of the hydroxypropyl cellulose matrix is presented. Good agreement between the quantitative model predictions and the experimental studies of Drug release was obtained. We achieved controlled release rates of multiple antiretrovirals ranging from μg/d to mg/d by altering the orifice design, Drug loading, and mass of pellets loaded in the device. This device could provide an adaptable platform for the Vaginal Drug Delivery of many molecules.
-
engineering a segmented dual reservoir polyurethane intraVaginal ring for simultaneous prevention of hiv transmission and unwanted pregnancy
PLOS ONE, 2014Co-Authors: Justin T. Clark, Meredith R. Clark, Namdev B. Shelke, Todd J. Johnson, Andrew K. Andreasen, Joel S. Nebeker, Judit Fabian, David R. Friend, Eric Smith, Patrick F KiserAbstract:The HIV/AIDS pandemic and its impact on women prompt the investigation of prevention strategies to interrupt sexual transmission of HIV. Long-acting Drug Delivery systems that simultaneously protect womenfrom sexual transmission of HIV and unwanted pregnancy could be important tools in combating the pandemic. We describe the design, in silico, in vitro and in vivo evaluation of a dual-reservoir intraVaginal ring that delivers the HIV-1 reverse transcriptase inhibitor tenofovir and the contraceptive levonorgestrel for 90 days. Two polyether urethanes with two different hard segment volume fractions were used to make coaxial extruded reservoir segments with a 100 µm thick rate controlling membrane and a diameter of 5.5 mm that contain 1.3 wt% levonorgestrel. A new mechanistic diffusion model accurately described the levonorgestrel burst release in early time points and pseudo-steady state behavior at later time points. As previously described, tenofovir was formulated as a glycerol paste and filled into a hydrophilic polyurethane, hollow tube reservoir that was melt-sealed by induction welding. These tenofovir-eluting segments and 2 cm long coaxially extruded levonorgestrel eluting segments were joined by induction welding to form rings that released an average of 7.5 mg tenofovir and 21 µg levonorgestrel per day in vitro for 90 days. Levonorgestrel segments placed intraVaginally in rabbits resulted in sustained, dose-dependent levels of levonorgestrel in plasma and cervical tissue for 90 days. Polyurethane caps placed between segments successfully prevented diffusion of levonorgestrel into the tenofovir-releasing segment during storage.Hydrated rings endured between 152 N and 354 N tensile load before failure during uniaxial extension testing. In summary, this system represents a significant advance in Vaginal Drug Delivery technology, and is the first in a new class of long-acting multipurpose prevention Drug Delivery systems.
-
state of the art in intraVaginal ring technology for topical prophylaxis of hiv infection
Aids Reviews, 2012Co-Authors: Patrick F Kiser, Todd J. Johnson, Justin T. ClarkAbstract:There is renewed interest in the development of long-term, controlled-release dosage forms for the intraVaginal Delivery of antiretrovirals for HIV prophylaxis. This interest has catalyzed a renaissance in Vaginal Drug Delivery, increasing the fundamental understanding of determinants of controlled Drug Delivery in the vagina as well as development of new materials, Delivery platforms, and animal models. Our goal in writing this review from the perspective of engineers and pharmaceutical scientists interested in prevention of sexually transmitted infections is to highlight the current state of the art, progress in preclinical programs, new Drug-Delivery device designs, and to discuss some of the important unknowns in this area of HIV prevention for the general audience involved in HIV research. As far as antiretrovirals are concerned, this review is limited to programs working with antiretrovirals that are supported with an investigational new Drug filing. We draw primarily from published papers in the PubMed and CAS databases, however, many of the most recent advances have yet to appear in the peer-reviewed literature and for this class of publications we draw from a recent formulation workshop held by CONRAD as well as from the Microbicides, Controlled Release Society, and CROI meetings.
-
design of a semisolid Vaginal microbicide gel by relating composition to properties and performance
Pharmaceutical Research, 2010Co-Authors: Alamelu Mahalingam, Meredith R. Clark, Judit Fabian, David R. Friend, Eric Smith, Festo Damian, Jennifer J Peters, David F Katz, Patrick F KiserAbstract:Purpose Develop a preclinical in vitro algorithm enabling de novo design of semisolid Vaginal Drug Delivery gels, by using biomechanical modeling of gel spreading in the Vaginal canal and empirically relating gel composition to mechanical properties and predicted performance.
-
design of a semisolid Vaginal microbicide gel by relating composition to properties and performance
Pharmaceutical Research, 2010Co-Authors: Alamelu Mahalingam, Meredith R. Clark, Judit Fabian, David R. Friend, Eric Smith, Festo Damian, Jennifer J Peters, David F Katz, Patrick F KiserAbstract:Develop a preclinical in vitro algorithm enabling de novo design of semisolid Vaginal Drug Delivery gels, by using biomechanical modeling of gel spreading in the Vaginal canal and empirically relating gel composition to mechanical properties and predicted performance. Gel performance was defined through a multivariate objective function constructed from gels’ mechanical properties and selected performance criteria for gel spreading within the Vaginal canal. Mixture design of experiment was used to establish a semi-empirical relationship linking composition-property and property-performance relationships for gels with varying concentrations of hydroxyethylcellulose and Carbopol 974P. This permits definition of a local optimum for gel composition and volume of administration, within a defined gel composition space. Rheological behavior and, consequently, the value of the objective function varied broadly with composition. The algorithm indicated a 3.0 wt% HEC gel as the near optimal composition for a 3.5 mL applied volume for gels designed to spread throughout the vagina. The algorithm introduced herein is a novel tool that facilitates an understanding of the composition-property-performance relationship for Vaginal semisolid Drug Delivery gels. This approach has promise as a scientific methodology for evaluation and optimization of Vaginal gels prior to in vivo investigations.
Guzel K Abilova - One of the best experts on this subject based on the ideXlab platform.
-
chitosan poly 2 ethyl 2 oxazoline films with ciprofloxacin for application in Vaginal Drug Delivery
Materials, 2020Co-Authors: Guzel K Abilova, Daulet B Kaldybekov, G S Irmukhametova, Diara S Kazybayeva, Zhanar A Iskakbayeva, Sarkyt E Kudaibergenov, Vitaliy V KhutoryanskiyAbstract:Chitosan (CHI) and chitosan/poly(2-ethyl-2-oxazoline) (CHI/POZ)-based films were prepared by casting from aqueous solutions of polymer blends with different compositions. Ciprofloxacin was used as a model Drug in these formulations. The weight, thickness, folding endurance and transparency of blend films were measured and characterised. All films had a uniform thickness (0.06 ± 0.01 mm) and exhibited sufficient flexibility. The surface pHs of films ranged from 3.76 ± 0.49 to 4.14 ± 0.32, which is within the pH range suitable for Vaginal applications. The cumulative release of the Drug from the films in experiments in vitro was found to be 42 ± 2% and 56 ± 1% for pure CHI and CHI/POZ (40:60) films, respectively. Drug-free chitosan/poly(2-ethyl-2-oxazoline) films showed weak antimicrobial activity against Escherichia coli. Drug-loaded CHI and CHI/POZ films showed good antimicrobial properties against both Gram-positive Staphylococcus aureus and Gram-negative bacteria Escherichia coli. Mucoadhesive properties of these films with respect to freshly excised sheep Vaginal mucosa were evaluated using a tensile method. It was established that all films were mucoadhesive, but an increase in POZ content in the blend resulted in a gradual reduction of their ability to stick to Vaginal mucosa. These films could potentially find applications in Vaginal Drug Delivery.
Fusun Acarturk - One of the best experts on this subject based on the ideXlab platform.
-
development and characterization of chitosan nanoparticles loaded nanofiber hybrid system for Vaginal controlled release of benzydamine
European Journal of Pharmaceutical Sciences, 2021Co-Authors: Fatmanur Tugcudemiroz, Sinem Saar, Adnan Altug Kara, Aysegul Yildiz, Emre Tuncel, Fusun AcarturkAbstract:Vaginal infections caused by various pathogens such as fungi, viruses and protozoa are frequently seen. Systemic and local treatments can be applied to eliminate these infections. Novel Vaginal Drug Delivery systems can be used to provide local treatment. Vaginal Drug Delivery systems prevent systemic side effects and can provide long-term Drug release in the Vaginal area. Nanofibers and nanoparticles have a wide range of applications and can also be preferred as Vaginal Drug Delivery systems. Benzydamine is a non-steroidal anti-inflammatory and antiseptic Drug which is used for treatment of Vaginal infections. The aim of this study was to compare the nanofiber and gel formulations containing lyophilized benzydamine nanoparticles with nanofiber and gel formulations containing free benzydamine, and to provide prolonged release for protection from the Vaginal infections. Ionic gelation method was used for the preparation of benzydamine loaded nanoparticles. To produce benzydamine nanoparticles loaded nanofiber formulations, polyvinylpyrrolidone (PVP) solutions were prepared at 10% concentrations and mixed with nanoparticles. Hydroxypropyl methylcellulose (HPMC) was used as a gelling agent at the concentration of 1% for the Vaginal gel formulation. Nanoparticles were characterized in terms of zeta potential, polydispersity index and particle size. Viscosity, surface tension and conductivity values of the polymer solutions were measured for the electrospinning. Mechanical properties, contact angle and Drug loading capacity of the fibers were determined. Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), transmission electron microscopy (TEM), fourier-transform infrared (FT-IR) spectroscopy, mucoadhesion, ex vivo permeability studies and in vitro release studies were performed for the selected formulations. Ex vivo permeability studies were performed using Franz diffusion cell method. SEM and TEM images showed that fiber diameters increased with loading of nanoparticles. DSC studies showed no interaction between excipients used in the formulation. Tensile strength and elongation at break values of the fibers increased with the loading of nanoparticles, and the contact angle values of the fibers were found to be 0°. Addition of benzydamine nanoparticles to gel and nanofiber formulations increased mucoadhesion compared to free benzydamine loading formulations. Benzydamine nanoparticle loaded gel and nanofiber formulations penetrated slower than that of free benzydamine gel and fiber formulations. The results demonstrated that benzydamine and benzydamine nanoparticle loaded fibers and gels could be a potential Drug Delivery system for the treatment of Vaginal infections. Chitosan nanoparticle loaded nanofiber formulations are offered as an alternative controlled release Vaginal formulations for Vaginal infections.
-
electrospun metronidazole loaded nanofibers for Vaginal Drug Delivery
Drug Development and Industrial Pharmacy, 2020Co-Authors: Fatmanur Tugcudemiroz, Sinem Saar, Serdar Tort, Fusun AcarturkAbstract:Objective: To develop and characterize innovative Vaginal dosage forms for the treatment of bacterial vaginosis (BV).Significance: This study is the first comparative evaluation of the metronidazole (MET)-loaded polyvinylpyrrolidone (PVP) nanofiber formulations on BV treatment. Vaginal nanofibers are one of the potential innovative dosage forms for BV treatment because of their flexible, mucoadhesive, and easy application in Vaginal application which can be applied by the mucosal route.Methods: Blank and MET-loaded PVP solutions were prepared at three different concentrations (10, 12.5, 15%) for produce nanofiber. The suitability of the viscosities, surface tensions, and conductivity values of the solutions used to produce nanofibers for the electrospinning process has been evaluated. Scanning electron microscopy, mucoadhesion, permeability, Fourier transform infrared spectroscopy, differential scanning calorimetry, and Drug release tests were performed to reveal the physical, chemical, and pharmaceutical properties of the nanofibers. Mechanical properties, and contact angle of the fibers were also determined. Gel and solution formulations containing MET were prepared for comparative studies.Results: All polymer solutions were found to be suitable for electrospinning process. PVP concentration directly affected nanofiber diameter, mechanical, and mucoadhesion properties of nanofibers. The release profiles of the Drug from the nanofibers were similar for all concentration of PVP and release from the fibers was rapid. The permeability coefficient of MET from nanofibers was increased more than gel and solution formulations.Conclusions: Vaginal use of MET-loaded nanofibers has been shown to be a potential Drug Delivery system for the treatment of BV.
-
mucoadhesive Vaginal Drug Delivery systems
Recent Patents on Drug Delivery & Formulation, 2009Co-Authors: Fusun AcarturkAbstract:Vaginal Delivery is an important route of Drug administration for both local and systemic diseases. The Vaginal route has some advantages due to its large surface area, rich blood supply, avoidance of the first-pass effect, relatively high permeability to many Drugs and self-insertion. The traditional commercial preparations, such as creams, foams, gels, irrigations and tablets, are known to reside in the Vaginal cavity for a relatively short period of time owing to the self-cleaning action of the Vaginal tract, and often require multiple daily doses to ensure the desired therapeutic effect. The Vaginal route appears to be highly appropriate for bioadhesive Drug Delivery systems in order to retain Drugs for treating largely local conditions, or for use in contraception. In particular, protection against sexually-transmitted diseases is critical. To prolong the residence time in the Vaginal cavity, bioadhesive therapeutic systems have been developed in the form of semi-solid and solid dosage forms. The most commonly used mucoadhesive polymers that are capable of forming hydrogels are synthetic polyacrylates, polycarbophil, chitosan, cellulose derivatives (hydroxyethycellulose, hydroxy-propylcellulose and hydroxypropylmethylcellulose), hyaluronic acid derivatives, pectin, tragacanth, carrageenan and sodium alginate. The present article is a comprehensive review of the patents related to mucoadhesive Vaginal Drug Delivery systems.
Sarkyt E Kudaibergenov - One of the best experts on this subject based on the ideXlab platform.
-
chitosan poly 2 ethyl 2 oxazoline films with ciprofloxacin for application in Vaginal Drug Delivery
Materials, 2020Co-Authors: Guzel K Abilova, Daulet B Kaldybekov, G S Irmukhametova, Diara S Kazybayeva, Zhanar A Iskakbayeva, Sarkyt E Kudaibergenov, Vitaliy V KhutoryanskiyAbstract:Chitosan (CHI) and chitosan/poly(2-ethyl-2-oxazoline) (CHI/POZ)-based films were prepared by casting from aqueous solutions of polymer blends with different compositions. Ciprofloxacin was used as a model Drug in these formulations. The weight, thickness, folding endurance and transparency of blend films were measured and characterised. All films had a uniform thickness (0.06 ± 0.01 mm) and exhibited sufficient flexibility. The surface pHs of films ranged from 3.76 ± 0.49 to 4.14 ± 0.32, which is within the pH range suitable for Vaginal applications. The cumulative release of the Drug from the films in experiments in vitro was found to be 42 ± 2% and 56 ± 1% for pure CHI and CHI/POZ (40:60) films, respectively. Drug-free chitosan/poly(2-ethyl-2-oxazoline) films showed weak antimicrobial activity against Escherichia coli. Drug-loaded CHI and CHI/POZ films showed good antimicrobial properties against both Gram-positive Staphylococcus aureus and Gram-negative bacteria Escherichia coli. Mucoadhesive properties of these films with respect to freshly excised sheep Vaginal mucosa were evaluated using a tensile method. It was established that all films were mucoadhesive, but an increase in POZ content in the blend resulted in a gradual reduction of their ability to stick to Vaginal mucosa. These films could potentially find applications in Vaginal Drug Delivery.
