scholarly journals A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 217 ◽  
Author(s):  
Ghada El-Zaafarany ◽  
Mahmoud Soliman ◽  
Samar Mansour ◽  
Marco Cespi ◽  
Giovanni Palmieri ◽  
...  
Keyword(s):  
Lactic Acid ◽  
Drug Release ◽  
Glycolic Acid ◽  
Histopathological Examination ◽  
Nasal Administration ◽  
Poly Lactic Acid ◽  
Saline Control ◽  
Pharmacokinetic Studies ◽  
Sustained Drug Release

The use of nanocarrier delivery systems for direct nose to brain drug delivery shows promise for achieving increased brain drug levels as compared to simple solution systems. An example of such nanocarriers is emulsomes formed from lipid cores surrounded and stabilised by a corona of phospholipids (PC) and a coating of Tween 80, which combines the properties of both liposomes and emulsions. Oxcarbazepine (OX), an antiepileptic drug, was entrapped in emulsomes and then localized in a poly(lactic acid-co-glycolic acid)-poly(ethylene glycol)-poly(lactic acid-co-glycolic acid) (PLGA-PEG-PLGA) triblock copolymer thermogel. The incorporation of OX emulsomes in thermogels retarded drug release and increased its residence time (MRT) in rats. The OX-emulsome and the OX-emulsome-thermogel formulations showed in vitro sustained drug release of 81.1 and 53.5%, respectively, over a period of 24 h. The pharmacokinetic studies in rats showed transport of OX to the systemic circulation after nasal administration with a higher uptake in the brain tissue in case of OX-emulsomes and highest MRT for OX-emulsomal-thermogels as compared to the IN OX-emulsomes, OX-solution and Trileptal® suspension. Histopathological examination of nasal tissues showed a mild vascular congestion and moderate inflammatory changes around congested vessels compared to saline control, but lower toxic effect than that reported in case of the drug solution.

scholarly journals Drug Release from Electrospun Poly(Lactic Acid) Membranes and Their Cell Viability in Vitro Test

2012 ◽  
Vol 44 ◽  
pp. 866-868 ◽  
Author(s):  
A.P.S. Immich ◽  
M. Lis ◽  
L.H. Catalani ◽  
R.L. Boemo ◽  
J.A. Tornero
Keyword(s):  
Lactic Acid ◽  
Drug Release ◽  
Cell Viability ◽  
Poly Lactic Acid ◽  
In Vitro Test ◽  
Vitro Test

scholarly journals Drug-Eluting Biodegradable Implants for the Sustained Release of Bisphosphonates

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2930
Author(s):  
Cintya Dharmayanti ◽  
Todd A. Gillam ◽  
Desmond B. Williams ◽  
Anton Blencowe
Keyword(s):  
Drug Release ◽  
Release Profile ◽  
Polymer Chains ◽  
Poly Lactic Acid ◽  
Initial Surface ◽  
Sustained Drug Release ◽  
Drug Eluting ◽  
Release In Vitro ◽  
Poor Absorption

Despite being one of the first-line treatments for osteoporosis, the bisphosphonate drug class exhibits an extremely low oral bioavailability (<1%) due to poor absorption from the gastrointestinal tract. To overcome this, and to explore the potential for sustained drug release, bioerodible poly(lactic acid) (PLA) and poly(D,L-lactide-co-glycolide) (PLGA) implants loaded with the bisphosphonate alendronate sodium (ALN) were prepared via hot-melt extrusion. The rate of drug release in vitro was modulated by tailoring the ratio of lactide to glycolide in the polymer and by altering the ALN-loading of the implants. All investigated implants exhibited sustained ALN release in vitro between 25 to 130 days, where implants of greater glycolide composition and higher ALN-loadings released ALN more rapidly. All PLGA implants demonstrated a sigmoidal release profile, characterised by an initial surface dissolution phase, followed by a period of zero-order drug diffusion, then relaxation or erosion of the polymer chains that caused accelerated release over the subsequent days. Contrastingly, the PLA implants demonstrated a logarithmic release profile, characterised by a gradual decrease in ALN release over time.

Development and Characterization of Binary Solid Lipid Nano Suspension of Atorvastatin: In-Vitro Drug Release and In-Vivo Pharmacokinetic Studies

2019 ◽  
Vol 11 (11) ◽  
pp. 1522-1530
Author(s):  
Mahwish Kamran ◽  
Mir Azam Khan ◽  
Muhammad Shafique ◽  
Maqsood ur Rehman ◽  
Waqar Ahmed ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
Drug Loading ◽  
Lipid Lowering ◽  
Diffusion Method ◽  
Pharmacokinetic Studies ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Solid Lipid

Atorvastatin is an extensively used lipid lowering agent. But the vital issue associated with it is low oral bioavailability (12%) owing to poor aqueous solubility. To overcome this tribulation, binary solid lipid nano suspension of Atorvastatin (ATO) was formulated by solvent diffusion method. The combination of stearic acid and oleic acid was utilized as a lipid carrier with Tween-80 (surfactant) along with Polyvinylpyrrolidone (co-surfactant). Optimized nano formulation was prepared by changing the formulation variables. Optimized nano suspension (ATO-4) represented particle size 228.3 ± 2.1 nm and polydispersity index (PDI) 0.225 ± 0.02 with zeta potential (ZP) – 33.6 ± 0.02 mV. Encapsulation efficiency along with drug loading capacity was 88.3 ± 2.5% and 4.9 ± 0.14% respectively. Scanning electron microscopic (SEM) analysis exposed spherical shaped amorphous particles. Differential scanning calorimetry (DSC) as well as X-ray powder diffraction (P-XRD) established reduction in drug's crystalline state. Fourier transform infrared (FTIR) spectroscopy exposed no interaction amongst the drug and formulation contents. In-vitro studies revealed sustained pattern of drug release. Stability studies confirmed refrigerated temperature as most suitable for storage of binary solid lipid nano suspension. Plasma concentration versus time curve ascertained 2.78-fold increase in oral bioavailability of ATO nano suspension compared to the marketed product (Lipitor®). Findings proposed desired improvement in oral bioavailability of ATO nano suspension with sustained drug release profile. Thus, binary solid lipid nano suspension could be utilized as an advanced drug delivery system for oral deliverance of hydrophobic drugs.

Synthesis and Kinetic Studies on Controlled Release of 6-Thioguanine Entrapped Polyethylene Glycol-Co-Polylactic Acid Polymer Nanoparticles

2011 ◽  
Vol 9 (1) ◽  
Author(s):  
Sathishkumar Kannaiyan ◽  
T.G.Ashwin Narayanan ◽  
P.Karthick Sarathy ◽  
Nagarjun Sudhakar ◽  
Rama Krishnan
Keyword(s):  
Gold Nanoparticles ◽  
Lactic Acid ◽  
Polyethylene Glycol ◽  
Controlled Release ◽  
Drug Release ◽  
Kinetic Equations ◽  
Kinetic Studies ◽  
Poly Lactic Acid ◽  
Average Size

Poly lactic acid-polyethylene glycol (PLA-co-PEG) copolyester was synthesized from oligomer of L-lactic acid and poly ethylene glycol (PEG) using stannous octoate as catalyst. 6-Thioguanine containing Poly lactic acid-polyethylene glycol (PLA-co-PEG) nanocapsules were prepared in the presence and absence of gold nanoparticles via the W/O/W emulsification solvent-evaporation method. The morphologies of prepared nanocapsules changed substantially because of the presence of gold nanoparticles. From SEM and TEM measurements, the average size of the polymer nanocapsules and gold nanoparticles were found to be in range of 230-260 nm and 18-20 nm, respectively. In general the drug release was quicker in Phosphate buffer saline (pH 7.4) compared to 0.1M hydrochloric acid and this may be due to higher solubility, higher swelling and penetration properties of PLA-co-PEG in PBS compared to HCl. Polymer nanocapsules with gold show a prolonged controlled release with higher encapsulation efficiency (75%) compared to that of polymer nanocapsules (45%) in the absence of gold nanoparticles. It may be due to the more entrapping efficiency of gold and less diffusivity of drugs from the nanocapsules. Application of in vitro drug release data to various kinetic equations indicated Higuchi model, indicating a uniform distribution of thioguanine in the nanocapsules.

scholarly journals DEGRADASI POLIBLEND POLI(ASAMLAKTAT-KO-ASAMGLIKOLAT) DENGAN POLI(ε-KAPROLAKTON) SECARA IN VITRO

2015 ◽  
Vol 2 (2) ◽  
pp. 174
Author(s):  
Tetty Kemala ◽  
Achmad Sjahriza ◽  
Hendra Adijuwana ◽  
Mardiana Hardianti
Keyword(s):  
Lactic Acid ◽  
Polylactic Acid ◽  
Intrinsic Viscosity ◽  
Phosphate Buffer ◽  
Glycolic Acid ◽  
Incubation Temperature ◽  
Human Life ◽  
Polyglycolic Acid ◽  
Poly Lactic Acid

 ABSTRACT  Polymer has many applications in human life, one of them is in the field of health. Polymer synthetics like polylactic acid (PLA), polyglycolic acid (PGA), poly(ε-caprolactone) (PCL), and poly(lactic acid-co-glycolic acid) (PLGA) were kind of polyesters that is many used in field   of health. Many researchers have already made research about degradation of PLA, PGA, PCL, and PLGA. However, there is no one doing research about degradation of combination between this two polymers, one of them is polyblend of  PLGA and PCL. Polyblend were made of four compositions, that were PLGA(90:10):PCL 3:1, PLGA(75:25):PCL 3:1, PLGA(90:10):PCL 5:1, and PLGA(75:25):PCL 5:1. Degradation was carried out for eight weeks by using phosphate buffer pH 7.4 and incubation temperature of 37°C. Degradation of the polymer was observed by mass remained, and intrinsic viscosity. The result showed that composition PLGA(75:25):PCL 5:1 was the fastest in degradation compared to other compositions. It was showed by the decrease in mass until 89.06% and the change in intrinsic viscosity until 20.13%. Keywords: PLGA, PCL   

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