scholarly journals Key Factor Study for Generic Long-Acting PLGA Microspheres Based on a Reverse Engineering of Vivitrol®

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1247
Author(s):  
Yabing Hua ◽  
Zengming Wang ◽  
Dan Wang ◽  
Xiaoming Lin ◽  
Boshi Liu ◽  
...  
Keyword(s):  
Reverse Engineering ◽  
Process Parameters ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Plga Microspheres ◽  
Factor Study ◽  
Key Factor ◽  
Process Factors ◽  
Long Acting

The FDA (U.S. Food and Drug Administration) has approved only a negligible number of poly(lactide-co-glycolide) (PLGA)-based microsphere formulations, indicating the difficulty in developing a PLGA microsphere. A thorough understanding of microsphere formulations is essential to meet the challenge of developing innovative or generic microspheres. In this study, the key factors, especially the key process factors of the marketed PLGA microspheres, were revealed for the first time via a reverse engineering study on Vivitrol® and verified by the development of a generic naltrexone-loaded microsphere (GNM). Qualitative and quantitative similarity with Vivitrol®, in terms of inactive ingredients, was accomplished by the determination of PLGA. Physicochemical characterization of Vivitrol® helped to identify the critical process parameters in each manufacturing step. After being prepared according to the process parameters revealed by reverse engineering, the GNM demonstrated similarity to Vivitrol® in terms of quality attributes and in vitro release (f2 = 65.3). The research on the development of bioequivalent microspheres based on the similar technology of Vivitrol® will benefit the development of other generic or innovative microspheres.

Study on in vitro release patterns of fentanyl-loaded PLGA microspheres

2003 ◽  
Vol 20 (5) ◽  
pp. 569-579 ◽  
Author(s):  
S.-A. Seo ◽  
G. Khang ◽  
J. M. Rhee ◽  
J. Kim ◽  
H. B. Lee
Keyword(s):  
In Vitro Release ◽  
Plga Microspheres ◽  
Vitro Release

Design and Evaluation of Long Acting Biodegradable PLGA Microspheres for Ocular Drug Delivery

2019 ◽  
Vol 10 ◽  
Author(s):  
Anjali Pandya ◽  
Rajani Athawale ◽  
Durga Puro ◽  
Geeta Bhagwat
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Degradation Products ◽  
Ex Vivo ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Rational Approach ◽  
Plga Microspheres ◽  
Long Acting

Background: The research work involves development of PLGA biodegradable microspheres loaded with dexamethasome for intraocular delivery. Objective: To design and evaluate long acting PLGA microspheres for ocular delivery of dexamethasone. Method: Present formulation involves the development of long acting dexamethasone loaded microspheres composed of a biodegradable controlled release polymer, Poly(D, L- lactide-co-glycolide) (PLGA), for the treatment of posterior segment eye disorders intravitreally. PLGA with monomer ratio of 50:50 of lactic acid to glycolic acid was used to achieve a drug release up to 45 days. Quality by Design approach was utilized for designing the experiments. Single emulsion solvent evaporation technique along with high pressure homogenization was used to facilitate formation of microspheres. Results: Particle size evaluation, drug content and drug entrapment efficiency were determined for the microspheres. Particle size and morphology was observed using Field Emission Gun-Scanning Electron Microscopy (FEG-SEM) and microspheres were in the size range of 1-5 μm. Assessment of drug release was done using in vitro studies and transretinal permeation was observed by ex vivo studies using goat retinal tissues. Conclusion: Considering the dire need for prolonged therapeutic effect in diseases of the posterior eye, an intravitreal long acting formulation was designed. Use of biodegradable polymer with biocompatible degradation products was a rational approach to achieve this aim. Outcome from present research shows that developed microspheres would provide a long acting drug profile and reduce the frequency of administration thereby improving patient compliance.

Preparation and characterization of fentanyl-loaded PLGA microspheres: in vitro release profiles

2002 ◽  
Vol 234 (1-2) ◽  
pp. 195-203 ◽  
Author(s):  
Hak Soo Choi ◽  
Sun-Ah Seo ◽  
Gilson Khang ◽  
John M. Rhee ◽  
Hai Bang Lee
Keyword(s):  
In Vitro Release ◽  
Plga Microspheres ◽  
Vitro Release ◽  
Release Profiles

Influence of drying processes on the structures, morphology and in vitro release profiles of risperidone-loaded PLGA microspheres

2019 ◽  
Vol 36 (1) ◽  
pp. 21-31 ◽  
Author(s):  
Zhaoying Wu ◽  
Mengqing Zhao ◽  
Wei Zhang ◽  
Zhao Yang ◽  
Shuxin Xu ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Plga Microspheres ◽  
Vitro Release ◽  
Release Profiles

scholarly journals Models and methods to characterise levonorgestrel release from intradermally administered contraceptives

2021 ◽  
Author(s):  
Adnan Al Dalaty ◽  
Benedetta Gualeni ◽  
Sion A. Coulman ◽  
James C. Birchall
Keyword(s):  
Ex Vivo ◽  
Extraction Procedure ◽  
In Vitro Release ◽  
Reversed Phase ◽  
Experimental Models ◽  
Detection Methods ◽  
Hormonal Contraceptives ◽  
Limit Of Quantification ◽  
Long Acting

AbstractMicroneedle (MN)-based technologies have been proposed as a means to facilitate minimally invasive sustained delivery of long-acting hormonal contraceptives into the skin. Intradermal administration is a new route of delivery for these contraceptives and therefore no established laboratory methods or experimental models are available to predict dermal drug release and pharmacokinetics from candidate MN formulations. This study evaluates an in vitro release (IVR) medium and a medium supplemented with ex vivo human skin homogenate (SH) as potential laboratory models to investigate the dermal release characteristics of one such hormonal contraceptive that is being tested for MN delivery, levonorgestrel (LNG), and provides details of an accompanying novel two-step liquid–liquid drug extraction procedure and sensitive reversed-phase HPLC–UV assay. The extraction efficiency of LNG was 91.7 ± 3.06% from IVR medium and 84.6 ± 1.6% from the medium supplemented with SH. The HPLC–UV methodology had a limit of quantification of 0.005 µg/mL and linearity between 0.005 and 25 µg/mL. Extraction and detection methods for LNG were exemplified in both models using the well-characterised, commercially available sustained-release implant (Jadelle®). Sustained LNG release from the implant was detected in both media over 28 days. This study reports for the first time the use of biologically relevant release models and a rapid, reliable and sensitive methodology to determine release characteristics of LNG from intradermally administered long-acting drug delivery systems. Graphical abstract

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals Phenobarbital loaded microemulsion: development, kinetic release and quality control

2016 ◽  
Vol 52 (2) ◽  
pp. 251-264 ◽  
Author(s):  
Kayo Alves Figueiredo ◽  
Jamilly Kelly Oliveira Neves ◽  
José Alexsandro da Silva ◽  
Rivelilson Mendes de Freitas ◽  
André Luis Menezes Carvalho
Keyword(s):  
Analytical Method ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Primary Stability ◽  
Isopropyl Myristate ◽  
Microemulsion System ◽  
Transdermal Application ◽  
Kinetics Of ◽  
Vitro Release

ABSTRACT This study aimed to obtain and characterize a microemulsion (ME) containing phenobarbital (PB). The PB was incorporated in the proportion of 5% and 10% in a microemulsion system containing Labrasol(r), ethanol, isopropyl myristate and purified water. The physicochemical characterization was performed and the primary stability of the ME was evaluated. An analytical method was developed using spectrophotometry in UV = 242 nm. The kinetics of the in vitro release (Franz model) of the ME and the emulsion (EM) containing PB was evaluated. The incorporation of PB into ME at concentrations of 5 and 10% did not change pH and resistance to centrifugation. There was an increase in particle size, a decrease of conductivity and a change in the refractive index in relation to placebo ME. The ME remained stable in preliminary stability tests. The analytical method proved to be specific, linear, precise, accurate and robust. Regarding the kinetics of the in vitro release, ME obtained an in vitro release profile greater than the EM containing PB. Thus, the obtained ME has a potential for future transdermal application, being able to compose a drug delivery system for the treatment of epilepsy.

Formulation development of matrix type transdermal patches containing mefenamic acid: physicochemical characterization and in vitro release evaluation

2017 ◽  
Vol 148 (7) ◽  
pp. 1215-1222 ◽  
Author(s):  
Jirapornchai Suksaeree ◽  
Kotchakorn Piamsap ◽  
Supawan Paktham ◽  
Tichakorn Kenprom ◽  
Chaowalit Monton ◽  
...  
Keyword(s):  
Mefenamic Acid ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Formulation Development ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Vitro Release

scholarly journals Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3512
Author(s):  
Mohammed F. Aldawsari ◽  
Md. Khalid Anwer ◽  
Mohammed Muqtader Ahmed ◽  
Farhat Fatima ◽  
Gamal A. Soliman ◽  
...  
Keyword(s):  
Sexual Behavior ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hydrophilic Polymers ◽  
Sildenafil Citrate ◽  
Male Rats ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Onset Of Action

Sildenafil citrate (SLC) is a frequently used medication (Viagra®) for the treatment of erectile dysfunction (ED). Due to its poor solubility, SLC suffers from a delayed onset of action and poor bioavailability. Hence, the aim of the proposed work was to prepare and evaluate solid dispersions (SDs) with hydrophilic polymers (Kolliphor® P188, Kollidon® 30, and Kollidon®-VA64), in order to enhance the dissolution and efficacy of SLC. The SLC-SDs were prepared using a solvent evaporation method (at the ratio drug/polymer, 1:1, w/w) and characterized by Differential Scanning Calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Scanning electron microscope (SEM), drug content, yield, and in vitro release studies. Based on this evaluation, SDs (SLC-KVA64) were optimized, with a maximum release of drug (99.74%) after 2 h for all the developed formulas. The SDs (SLC-KVA64) were further tested for sexual behavior activity in male rats, and significant enhancements in copulatory efficiency (81.6%) and inter-copulatory efficiency (44.9%) were noted in comparison to the pure SLC drug, when exposed to the optimized SLC-KVA64 formulae. Therefore, SD using Kollidon®-VA64 could be regarded as a potential strategy for improving the solubility, in vitro dissolution, and therapeutic efficacy of SLC.

Sign in / Sign up

Export Citation Format

Share Document