scholarly journals Design and Characterizations of Inhalable Poly(lactic-co-glycolic acid) Microspheres Prepared by the Fine Droplet Drying Process for a Sustained Effect of Salmon Calcitonin

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1311 ◽  
Author(s):  
Hideyuki Sato ◽  
Aiko Tabata ◽  
Tatsuru Moritani ◽  
Tadahiko Morinaga ◽  
Takahiro Mizumoto ◽  
...  
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Salmon Calcitonin ◽  
Glycolic Acid ◽  
Pharmacological Action ◽  
Conformational Structure ◽  
Intratracheal Administration ◽  
Fine Droplet ◽  
Droplet Drying

The present study aimed to develop inhalable poly (lactic-co-glycolic acid) (PLGA)-based microparticles of salmon calcitonin (sCT) for sustained pharmacological action by the fine droplet drying (FDD) process, a novel powderization technique employing printing technologies. PLGA was selected as a biodegradable carrier polymer for sustained-release particles of sCT (sCT/SR), and physicochemical characterizations of sCT/SR were conducted. To estimate the in vivo efficacy of the sCT/SR respirable powder (sCT/SR-RP), plasma calcium levels were measured after intratracheal administration in rats. The particle size of sCT/SR was 3.6 µm, and the SPAN factor, one of the parameters to present the uniformity of particle size distribution, was calculated to be 0.65. In the evaluation of the conformational structure of sCT, no significant changes were observed in sCT/SR even after the FDD process. The drug release from sCT/SR showed a biphasic pattern with an initial burst and slow diffusion in simulated lung fluid. sCT/SR-RP showed fine inhalation performance, as evidenced by a fine particle fraction value of 28% in the cascade impactor analysis. After the insufflation of sCT samples (40 µg-sCT/kg) in rats, sCT/SR-RP could enhance and prolong the hypocalcemic action of sCT possibly due to the sustained release and pulmonary absorption of sCT. From these observations, the strategic application of the FDD process could be efficacious to provide PLGA-based inhalable formulations of sCT, as well as other therapeutic peptides, to enhance their biopharmaceutical potentials.

In vivo assessment of salmon calcitonin sustained release from biodegradable microspheres

1991 ◽  
Vol 17 (2) ◽  
pp. 199-205 ◽  
Author(s):  
K.C. Lee ◽  
E.E. Soltis ◽  
P.S. Newman ◽  
K.W. Burton ◽  
R.C. Mehta ◽  
...  
Keyword(s):  
Sustained Release ◽  
Salmon Calcitonin ◽  
Biodegradable Microspheres ◽  
In Vivo Assessment

scholarly journals Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 168
Author(s):  
Md. Khalid Anwer ◽  
Essam A. Ali ◽  
Muzaffar Iqbal ◽  
Mohammed Muqtader Ahmed ◽  
Mohammed F. Aldawsari ◽  
...  
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Janus Kinase ◽  
Hybrid Nanoparticles ◽  
Polymer Hybrid ◽  
Vitro Release

Baricitinib (BTB) is an orally administered Janus kinase inhibitor, therapeutically used for the treatment of rheumatoid arthritis. Recently it has also been approved for the treatment of COVID-19 infection. In this study, four different BTB-loaded lipids (stearin)-polymer (Poly(d,l-lactide-co-glycolide)) hybrid nanoparticles (B-PLN1 to B-PLN4) were prepared by the single-step nanoprecipitation method. Next, they were characterised in terms of physicochemical properties such as particle size, zeta potential (ζP), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL). Based on preliminary evaluation, the B-PLN4 was regarded as the optimised formulation with particle size (272 ± 7.6 nm), PDI (0.225), ζP (−36.5 ± 3.1 mV), %EE (71.6 ± 1.5%) and %DL (2.87 ± 0.42%). This formulation (B-PLN4) was further assessed concerning morphology, in vitro release, and in vivo pharmacokinetic studies in rats. The in vitro release profile exhibited a sustained release pattern well-fitted by the Korsmeyer–Peppas kinetic model (R2 = 0.879). The in vivo pharmacokinetic data showed an enhancement (2.92 times more) in bioavailability in comparison to the normal suspension of pure BTB. These data concluded that the formulated lipid-polymer hybrid nanoparticles could be a promising drug delivery option to enhance the bioavailability of BTB. Overall, this study provides a scientific basis for future studies on the entrapment efficiency of lipid-polymer hybrid systems as promising carriers for overcoming pharmacokinetic limitations.

scholarly journals Formulasi dan Karakterisasi Nanopartikel Kafein Hasil Isolasi dari Biji Kopi Robusta

2021 ◽  
Vol 7 (1) ◽  
pp. 47-59
Author(s):  
Yunida Yunida ◽  
Muhammad Totong Kamaluddin ◽  
Theodorus Theodorus ◽  
Sonlimar Mangunsong
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Particle Size ◽  
Sustained Release ◽  
Vinyl Alcohol ◽  
Glycolic Acid ◽  
Polydispersity Index ◽  
Poly Vinyl Alcohol ◽  
Transmission Electron ◽  
Particle Size Analyzer

Kopi robusta merupakan jenis kopi yang paling banyak dikembangkan oleh petani di Indonesia. Kopi kaya akan zat bioaktif yang memberikan manfaat bagi kesehatan, salah satunya adalah kafein. Namun, konsumsi kafein dalam jumlah berlebihan juga dapat menimbulkan efek samping. Salah satu upaya untuk meminimalkan efek samping dan menghasilkan sediaan sustained release adalah dengan membuat formulasi kafein dalam bentuk sediaan nanopartikel. Dalam penelitian ini dilakukan ekstraksi, isolasi dan identifikasi kafein dari biji kopi robusta. Dari 200 gram biji kopi robusta diperoleh kristal kafein sebanyak 0,83 gram. Hasil identifikasi secara mikroskopis diperoleh morfologi kristal kafein seperti jarum-jarum panjang dan karakteristik kristal kafein mirip dengan kafein standar. Preparasi nanopartikel kafein dilakukan menggunakan metode single emulsion-solvent evaporation dengan pembawa PLGA (Poly-(Lactic-co-Glycolic Acid)) dan PVA (Poly(Vinyl Alcohol)) sebagai stabilizer. Karakterisasi preparat nanopartikel menggunakan PSA (Particle Size Analyzer) memberikan hasil diameter ukuran partikel 183,9 nm, nilai PDI (Polydispersity Index) 0,113 dan zeta potensial -13,5 mV. Penentuan morfologi menggunakan Transmission Electron Microscopy diperoleh partikel yang berbentuk bulat (spheris).  

Formulation optimization and in vitro characterization of granisetron-loaded polylactic-co-glycolic acid microspheres prepared by a dropping-in-liquid emulsification technique

2021 ◽  
Vol 18 ◽  
Author(s):  
Atef Mohammed Qasem Ahmed ◽  
Li-Qing Chen ◽  
Huan-Huan Du ◽  
Wei Sun ◽  
Qing-Ri Cao
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Molecular Interactions ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Plga Microspheres ◽  
Scanning Calorimetry ◽  
Medium Ph ◽  
Hardening Process

Purpose: Traditional dosage forms of granisetron (GRN) decrease patient compliance associated with repeated drug administration because of the short half-life of the drug. Methods: In this study, novel GRN-loaded polylactic-co-glycolic acid (PLGA) sustained release microspheres were prepared for the first time via a dropping-in-liquid emulsification technique. The effect of various factors, such as pH of the outer phase, Tween80, polyvinyl alcohol (PVA) concentrations, and hardening process, on the encapsulation efficiency (EE), drug loading (DL), and particle size of microspheres were extensively studied. The physicochemical properties, including drug release, surface morphology, crystallinity, thermal changes, and molecular interactions, were also studied. Results: GRN has a pH-dependent solubility and showed a remarkably high solubility under an acidic condition. The EE of the alkaline medium (pH 8) was higher than that of the acidic medium (pH 4.0). EE and DL decreased in the presence of Tween80 in the outer phase, whereas EE significantly increased during hardening. The particle size of microspheres was not affected by PVA and Tween80 concentrations, but it was influenced by PVA volume and hardening. X-ray diffraction and differential scanning calorimetry results showed that the physical state of the drug changed from a crystalline form to an amorphous form, thereby confirming that the drug was encapsulated into the PLGA matrix. Fourier transform-infrared spectroscopy confirmed that some molecular interactions occurred between the drug and the polymer. GRN-loaded PLGA microspheres showed sustained release profiles of over 90% on week 3. Conclusion: GRN-loaded PLGA microspheres with sustained release were successfully prepared, and they exhibited a relatively high EE without Tween 80 as an emulsifier and with hardening process.

Sustained release of salmon calcitonin in vivo from lactide: Glycolide copolymer depots

1993 ◽  
Vol 52 (5) ◽  
pp. 361-364 ◽  
Author(s):  
A. J. Millest ◽  
J. R. Evans ◽  
J. J. Young ◽  
D. Johnstone
Keyword(s):  
Sustained Release ◽  
Salmon Calcitonin

In vivo sustained release of adenoviral vectors from poly(d,l-lactic-co-glycolic) acid microparticles prepared by TROMS

2004 ◽  
Vol 94 (1) ◽  
pp. 229-235 ◽  
Author(s):  
Guillermo Garcı́a del Barrio ◽  
Joanna Hendry ◽  
M.J Renedo ◽  
Juan M Irache ◽  
Francisco J Novo
Keyword(s):  
Sustained Release ◽  
Glycolic Acid ◽  
Adenoviral Vectors

Enhanced Stability and Controlled Delivery of MOF Encapsulated Vaccines and Their Immunogenic Response In Vivo

2018 ◽  
Author(s):  
Michael Luzuriaga ◽  
Raymond P. Welch ◽  
Madushani Dharmawardana ◽  
Candace Benjamin ◽  
Shaobo Li ◽  
...  
Keyword(s):  
Viral Vector ◽  
Controlled Delivery ◽  
Conformational Structure ◽  
Spectroscopy Analysis ◽  
Zeolitic Imidazolate Framework ◽  
Structural Conformation ◽  
Depth Study ◽  
Viral Nanoparticle

<div><div><div><p>Vaccines have an innate tendency to lose their structural conformation upon environmental and chemical stressors. A loss in conformation reduces the therapeutic ability to prevent the spread of a pathogen. Herein, we report an in-depth study of zeolitic imidazolate framework-8 (ZIF-8) and its ability to provide protection for a model viral vector against dena- turing conditions. The immunoassay and spectroscopy analysis together demonstrate enhanced thermal and chemical stability to the conformational structure of the encapsulated viral nanoparticle. The long-term biological activity of this virus-ZIF composite was investigated in animal models to further elucidate the integrity of the encapsulated virus, the bio-safety, and immunogenicity of the overall composite. Additionally, histological analysis found no observable tissue damage in the skin or vital organs in mice, following multiple subcutaneous administrations. This study shows that ZIF-based protein composites are strong candidates for improved preservation of proteinaceous drugs, are biocompatible, and capable of controlling the release and adsorption of drugs in vivo.</p></div></div></div>

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

Development of Sustained Release Multi-Component Microparticulate System of Diclofenac Sodium and Tizanidine Hydrochloride

1970 ◽  
Vol 1 (1) ◽  
pp. 97-105
Author(s):  
Kamlesh Dashora ◽  
Shailendra Saraf ◽  
Swarnalata Saraf
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Cellulose Acetate ◽  
Rate Constant ◽  
Diclofenac Sodium ◽  
Order Rate Constant ◽  
Anomalous Transport ◽  
First Order ◽  
Sem Study ◽  
Transport Type

Sustained released tablets of diclofenac sodium (DIC) and tizanidine hydrochloride (TIZ) were prepared by using different proportions of cellulose acetate (CA) as the retardant material. Nine formulations of tablets having different proportion of microparticles developed by varied proportions of polymer: drug ratio ‘’i.e.’’; 1:9 -1:3 for DIC and 1:1 – 3:1 for TIZ. Each tablet contained equivalent to 100 mg of DIC and 6mg of TIZ. The prepared microparticles were white, free flowing and spherical in shape (SEM study), with  the particle size varying from 78.8±1.94 to 103.33±1.28 µm and 175.92± 9.82 to 194.94±14.28µm for DIC  and TIZ, respectively.  The first order rate constant K1 of formulations were found to be in the range of  K1 = 0.117-0.272 and 0.083- 0.189 %hr-1for DIC and TIZ, respectively. The value of exponent coefficient (n) was found to be in the range of 0.6328-0.9412  and 0.8589-1.1954 for DIC and TIZ respectively indicates anomalous  to  non anomalous transport type of diffusions among different formulations

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