scholarly journals Development of size-tunable polymeric nanoparticles for drug delivery applications

2017 ◽  
Vol 1 (2) ◽  
pp. 31 ◽  
Author(s):  
Komkrich Sawasdee ◽  
Ployphailin Choksawad ◽  
Sopida Pimcharoen ◽  
Kanlaya Prapainop

Background:  Poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) have been widely used in drug delivery applications because of its excellent properties such as biocompatibility, biodegradability along with its abilities to deliver hydrophobic drugs, increase drug bioavailability, and improve drug absorption to targeted cells in both oral and parenteral administrations. The PLGA NPs can be synthesized using emulsion solvent evaporation method. Each parameter during synthesis play a role in formation of nanoparticles and could affect to form different NP sizes which is an important factor for successful development of drug delivery system.  Aims: The aim of this study is to prepare different sizes of PLGA NPs by investigation of four factors (molecular weight (MW) of PLGA, emulsifier concentrations, organic solvent type and power of ultrasonication) that involve in PLGA nanoparticle synthesis.Methods: PLGA nanoparticles were prepared by emulsion solvent evaporation method. Size and size distribution were analyzed by dynamic light scattering and polydispersity index (PdI).Results: The effect of four parameters: PLGA MW, emulsifier concentrations, solvent types, and amplitude of ultrasonication on PLGA NPs preparation were evaluated. Changing one parameter results in different sizes of PLGA NPs varied from 150-300 nm. PdI which is an indicator for determination of size distribution of NPs are also varied with overall value less than 0.2.Conclusion: MW of PLGA polymer, emulsifier concentration, type of organic solvent and power of ultrasonication affect the size and size distribution of PLGA NPs. 

2020 ◽  
Vol 14 (1) ◽  
pp. 75-89 ◽  
Author(s):  
Sandip Pawar ◽  
Pravin Shende

Background: : Currently, the most important challenge in the development of therapeutics and actives is their poor aqueous solubility and bioavailability. Objective: : The low aqueous solubility, poor pharmacokinetic properties, and bioavailability associated with novel actives manifest in numerous challenges in the formulation of conventional dosage forms like tablets, capsules, suspensions, emulsions, etc. Nanosponges are a novel class of drug delivery system capable of encapsulating or entrapping both lipophilic and hydrophilic drugs. Target-specific drug delivery and controlled drug release are the advantages offered by nanosponges which make them a promising anti-tumor drug delivery system. Methods: Nanosponges are colloidal structures comprising solid nanoparticles with cavities and meshlike structures for encapsulation of wide varieties of substances like antineoplastic agents, proteins and peptides, volatile oils, genetic material, etc. The methods of preparation of β-cyclodextrin-based nanosponges include solvent evaporation method, emulsion solvent evaporation method, ultrasound-assisted synthesis, hyper cross-linked cyclodextrin and interfacial phenomenon method. A large variety of nanosponges- based formulations are available in the market and some formulations of prostavastin, brexin, glymesason, mena-gargle, etc. are under clinical trials. Results: : Nanosponges possess potential applications in target site-specific drug delivery to liver, spleen, and lungs. Due to the surface functionalization, nanosponges show broad applications in water purification, protein delivery, chemical sensors, detection of explosives, agriculture, etc. In the near future, nanosponges-based products will capture a huge market for commercialization due to their improved properties and advantages. Conclusion: : This review provides an account of the patents related to nanosponges (2006-2018) and covers the broad applications of β-cyclodextrin-based nanosponges, their roles in vaccine delivery, cancer therapy, fire engineering, water purification, etc.


2019 ◽  
Vol 69 (7) ◽  
pp. 467-475
Author(s):  
Esmeralda Villicaña-Molina ◽  
Edith Pacheco-Contreras ◽  
Ena Athenea Aguilar-Reyes ◽  
Carlos Alberto León-Patiño

2018 ◽  
Vol 3 (1) ◽  
pp. 19
Author(s):  
Elfia Neswita ◽  
Elfi Sahlan Ben ◽  
Rahmi Nofita

<p>Telah dilakukan penelitian tentang mikroenkapsulasi atenolol dengan penyalut albumin menggunakan metode penguapan pelarut dan perbandingan atenolol dengan penyalut albumin yang digunakan adalah 1:1, 1:2 dan 1:3 berturut-turut untuk Formula I, Formula II dan Formula III. Mikrokapsul yang dihasilkan dievaluasi berdasarkan bentuk mikroskopis, distribusi ukuran partikel, penetapan kadar atenolol dalam mikrokapsul dan uji disolusi. Hasil foto mikroskopis menunjukkan mikrokapsul yang dihasilkan berbentuk sferis. Mikrokapsul mempunyai distribusi ukuran partikel 212-2000µm. Data penetapan kadar zat aktif dari masing-masing formula digunakan spektrofotometer UV dengan pelarut metanol dan  diperoleh kadar zat aktif  56,963 ± 17,589; 60,410 ± 1,005; 60,173 ± 1,016 % berturut-turut dalam formula I, Formula II, Formula III. Hasil disolusi menunjukkan bahwa semakin besar konsentrasi albumin pelepasan zat aktif dari mikrokapsul akan semakin diperlambat. Hasil penelitian menunjukkan bahwa mikrokapsul dengan perbandingan antara atenolol dengan albumin 1:1 memiliki pelepasan zat aktif yang paling baik. Kinetika pelepasan bahan aktif dari mikrokapsul mengikuti persamaan Korsmeyer Peppas dan Higuchi</p><p><em>The study about microencapsulation of atenolol with albumen as coating agent and by using solvent evaporation method had be done. The ratio atenolol and albumen were 1:1, 1:2 and 1:3 for Formula I, Formula II and Formula III respectively. The microencapsulation produced was evaluated by measuring microscopic, form particle size distribution, active compound released. The result of photo microscopic showed that microcapsules had spherical form. Microcapsules had particle size distribution between 212-2000 µm. The Spectrophotometer UV in methanol was used to measured the activate compound concentration of microcapsules and was got 56,963 ± 17,589; 60,41 ± 1,0045; 60 and 173 ± 1,0160 % for formula I, Formula II and Formula III. The result of this study showed that microcapsules with comparison between atenolol and albumen 1:1 had better release of active compound. Kinetic of atenolol released from microcapsule followed the Korsmeyer-Peppas and Higuchi.</em></p>


2019 ◽  
Vol 9 (01) ◽  
pp. 21-26
Author(s):  
Arif Budiman ◽  
Ayu Apriliani ◽  
Tazyinul Qoriah ◽  
Sandra Megantara

Purpose: To develop glibenclamide-nicotinamide cocrystals with the solvent evaporation method and evaluate their solubility and dissolution properties. Methods: Cocrystals of glibenclamide-nicotinamide (1:2) were prepared with the solvent evaporation method. The prediction of interactive cocrystals was observed using in silico method. The solubility and dissolution were performed as evaluation of cocrystals. The cocrystals also were characterized by differential scanning calorimetry (DSC), infrared spectrophotometry, and powder X-ray diffraction (PXRD). Result: The solubility and dissolution profile of glibenclamide-nicotinamide cocrystal (1:2) increased significantly compared to pure glibenclamide as well as its physical mixture. Characterization of cocrystal glibenclamide-nicotinamide (1:2) including infrared Fourier transform, DSC, and PXRD, indicated the formation of a new solid crystal phase differing from glibenclamide and nicotinamide. Conclusion: The confirmation of cocrystal glibenclamide-nicotinamide (1:2) indicated the formation of new solid crystalline phases that differ from pure glibenclamide and its physical mixture


Author(s):  
Adel M. Aly ◽  
Ahmed S. Ali

: Glipizide (GZ) is an oral blood-glucose-lowering drug of the sulfonylurea class characterized by its poor aqueous solubility. Aiming for the production of GZ tablets with rapid onset of action followed by prolonged effect; GZ-Polyethylene glycol (PEG 4000 and 6000) solid dispersions with different ratios, (using melting and solvent evaporation method), as well as, coprecipitate containing GZ with polymethyl-methacrylate (PMMA) were prepared. Four tablet formulations were prepared containing; a) GZ alone, b) GZ: PEG6000, 1:10, c) GZ:PMMA 1:3, and, d)both GZ:PEG6000 1:10 and GZ:PMMA 1:3. The solvent evaporation method showed more enhancement of GZ solubility than the melting one, and this solubilizing effect increased with PEG increment. Generally, PEG6000 showed more enhancement of dissolution than PEG4000 especially at 1:10 drug: polymer ratio (the most enhancing formula). Also, the prepared tablet formulations showed acceptable physical properties according to USP/NF requirements. The dissolution results revealed that tablets containing PEG6000 (1:10) have the most rapid release rate, followed by the formula containing both PEG6000 and PMMA, while that including PMMA alone showed the slowest dissolution rate. Moreover, In-vivo studies for each of the above four formulations, were performed using four mice groups. The most effective formula in decreasing the blood glucose level, through the first 6 hours, was that containing GZ and PEG6000, 1:10. However, formula containing the combination of enhanced and sustained GZ was the most effective in decreasing the blood glucose level through 16 hours. Successful in-vitro in-vivo correlations could be detected between the percent released and the percent decreasing of blood glucose level after 0.5 hours.


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