scholarly journals PREPARATION AND CHARACTERIZATION OF CHITOSAN NANOPARTICLES OF INSULIN FOR NASAL DELIVERY

2018 ◽  
Vol 8 (5-s) ◽  
pp. 400-406 ◽  
Author(s):  
Subhendu Sekhar Mishra ◽  
Ashish Sharma

The aim of this study was to prepare and evaluate nanoparticles containing insulin in different polymer ratio by ionotropic gelation method. The average particle size was found to be 130.4±3.4 -155.5±6.4nm. SEM indicates that nanoparticles have shown smooth and spherical shape. The zeta potential of optimized formulation was 35.5 mv which indicates moderate stability with no agglomeration. The average drug content was found to be 130.4±3.4 -155.5±6.4nm. The in vitro drug release data was analyzed using zero order, first order, Higuchi, and Korsmeyer-Peppas models. It was observed the best fit model for nanoparticles was higuchi model. The developed formulation in situ polymeric gel is designed in such a way that the gel will load insulin in higher concentration and it will also contain penetration enhancer which will enhance the absorption of release drug from gel to systemic circulation. Keywords: Insulin, Nanoparticle, invitro drug release study.

2019 ◽  
Vol 2019 ◽  
pp. 1-7 ◽  
Author(s):  
Niu Niu ◽  
Shu-Hua Teng ◽  
Hua-Jian Zhou ◽  
Hai-Sheng Qian

Chitosan-silica (CS-SiO2) hybrid microspheres were prepared through the combined process of sol-gel and emulsification-crosslinking. Their composition, morphology, in vitro bioactivity, and drug release behavior were investigated. The results showed that, when 20 wt% SiO2 was incorporated, the as-prepared CS-SiO2 hybrid microspheres exhibited a regular spherical shape, a high dispersity, and a uniform microstructure. Their average particle diameter was determined to be about 24.0 μm. The in situ deposited inorganic phase of the hybrid microspheres was identified as amorphous SiO2, and its actual content was determined by the TG analysis. As compared with the pure chitosan microspheres, the CS-SiO2 hybrid microspheres displayed a greatly improved in vitro bioactivity. Vancomycin hydrochloride (VH) was selected as a model drug. It was demonstrated that the CS-SiO2 hybrid microspheres presented a good capacity for both loading and sustained release of VH. Moreover, the increase of the SiO2 content efficiently slowed down the drug release rate of the CS-SiO2 hybrid microspheres.


2019 ◽  
Vol 9 (2) ◽  
pp. 89-96
Author(s):  
Abbaraju Krishna Sailaja ◽  
Juveria Banu

Aim: The aim of this investigation was to develop and characterize naproxen loaded chitosan nanoparticles by emulsion interfacial reaction method. Methodology: For emulsion interfacial reaction method chitosan was used as a polymer. In this method, eight formulations were prepared by varying drug to polymer concentration. Discussion: Out of eight formulations prepared using emulsion interfacial reaction method EI8 formulation was found to be the best formulation. The drug content was observed as 94.4%, entrapment efficiency and loading capacity were found to be 87.5% and 75%, respectively. The mean particle diameter was measured as 324.6nm and the Zeta potential value was found to be -42.4mv. In vitro drug release data showed 97.2% of drug release rate sustained up to 12hrs. Conclusion: The results clearly reveal that EI8 formulation having the highest amount of drug was considered as the best formulation because of its small mean particle diameter, good entrapment efficiency, and stability.


Author(s):  
Kumar Nishchaya ◽  
Swatantra K.S. Kushwaha ◽  
Awani Kumar Rai

Background: Present malignant cancer medicines has the advancement of magnetic nanoparticles as delivery carriers to magnetically accumulate anticancer medication in malignant growth tissue. Aim: In the present investigation, a silica nanoparticles (MSNs) stacked with hydroxyurea were combined and was optimized for dependent and independent variables. Method: In this study, microporous silica nanoparticle stacked with neoplastic medication had been prepared through emulsification followed with solvent evaporation method. Prepared MSNs were optimized for dependent and independent variables. Different formulations were prepared with varying ratio of polymer, lipid and surfactant which affects drug release and kinetics of drug release pattern. The obtained MSNs were identified by FTIR, SEM, drug entrapment, in-vitro drug release, drug release kinetics study, stability testing in order to investigate the nanoparticle characteristics. Results: The percentage drug entrapment of the drug for the formulations F1, F2, F3, was found to be 27.78%, 65.52% and 48.26%. The average particle size for F2 formulation was found to be 520 nm through SEM. The cumulative drug release for the formulations F1, F2, F3 was found to be 64.17%, 71.82% and 32.68%. The formulations were found to be stable which gives controlled drug delivery for 6 hours. Conclusion: From the stability studies data it can be culminated that formulations are most stable when stored at lower temperature or in refrigerator i.e. 5˚C ± 3˚C. It can be concluded that MSN’s loaded with hydroxyurea is a promising approach towards the management of cancer due to its sustained release and less side effects.


2018 ◽  
Vol 13 (2) ◽  
pp. 111 ◽  
Author(s):  
Yadi Suryadi ◽  
Tri Puji Priyatno ◽  
I Made Samudra ◽  
Dwi Ningsih Susilowati ◽  
Tuti Septi Sriharyani ◽  
...  

<p>Anthracnose (Colletotrichum gloeosporioides) is one of the important diseases of fruit crops that need to be controlled. This study was aimed to obtain the best formula of hydrolyzed nano chitosan and its potensial in controlling anthracnose. The hydrolyzed chitosan was prepared using chitinase enzyme extracted from Burkholderia cepacia isolate E76. Chitosan nanoparticles were synthesized using ionic gelation method by reacting hydrolyzed chitosan (0.2%) with Sodium tripolyphosphate (STPP) (0.1%) as cross-linking agent using 30&amp;ndash;60 minutes stirring condition. The bioactivity of the nano chitosan formula was tested to C. gloeosporioides under in vitro and in vivo assays. The specific enzymatic activity of the purified chitinase was higher (0.19 U/mg) than that of crude enzyme (supernatant) with the purity increased by 3.8 times. Of the four formula tested, Formula A (hydrolyzed chitosan to STPP volume ratio of 5 : 1 with 60 minutes stirring condition) was found good in terms of physical characteristic of the particle. The formula nano chitosan particle had the spherical-like shape with an average particle size of 126.2+3.8 nm, polydispersity index (PI) of 0.4+0.02, and zeta potential (ZP) value of 27.8+0.2 mV. Nano chitosan had an inhibitory activity to C. gloeosporioides in vitro up to 85.7%. Moreover, it could inhibit 61.2% of C. gloeosporioides spores germination. It was shown that nano chitosan was also effective to reduce anthracnose disease severity in vivo when applied as a preventive measure on chili and papaya fruits. This study could be used as a reference for further fruit coating application using nano chitosan as a promising postharvest biocontrol agent to C. gloeosporioides.</p>


Author(s):  
Nilesh S. Kulkarni ◽  
Mukta A. Kulkarni ◽  
Rahul H. Khiste ◽  
Mohini C. Upadhye ◽  
Shashikant N. Dhole

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.


2020 ◽  
Vol 10 ◽  
pp. 184798042091151 ◽  
Author(s):  
Ping Song ◽  
Wuchen Du ◽  
Wanzhen Li ◽  
Longbao Zhu ◽  
Weiwei Zhang ◽  
...  

Polymerized polypeptide nanomicelles have attracted much attention as novel drug carriers because of their good biocompatibility and degradability. To prepare doxorubicin (DOX)-loaded nanomicelles, an amphiphilic peptide, FFHFFH-KKGRGD (P12), was synthesized by solid-phase synthesis, and the physicochemical and drug-release properties, as well as the cytotoxicity of the nanomicelles, were evaluated in vitro. The P12-DOX polymer micelles were prepared by dialysis. The morphology and particle size were characterized by transmission electron microscopy and dynamic light scattering. The critical micelle concentration (CMC) of the polymer was determined by the probe method, and the drug-release characteristics of the micelles were studied by dynamic dialysis. The cytotoxicity and uptake of the P12-DOX micelles were evaluated against mouse breast cancer cells (4T1) and human umbilical vein endothelial cells. The peptide polymer micelles containing DOX were uniformly sized and had a spherical core–shell structure with an average particle size of 128.6 nm. The CMC of the polymer was low (0.0357 mg/mL). The in vitro release of DOX from the micelles is slow and is consistent with first-order kinetics. The copolymer micelles of the P12 polypeptide and DOX can be used as nanoscale spherical carriers of hydrophobic drugs and have broad applicability.


2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Fernanda Malaquias Barboza ◽  
Willian Moreira Machado ◽  
Luiz Renato Olchanheski Junior ◽  
Josiane Padilha de Paula ◽  
Sônia Faria Zawadzki ◽  
...  

Microparticles of poly(ε-caprolactone) (PCL) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing manidipine dihydrochloride (MAN) were successfully prepared by the simple emulsion/solvent evaporation method. All formulations showed loading efficiency rates greater than 80% and average particle size less than 8 μm. Formulations had spherical shape with smooth and porous surface for PCL and PHBV, respectively. According to Fourier-transform infrared spectroscopy, initial components were not chemically modified during microencapsulation. X-ray diffraction patterns and differential scanning calorimetry demonstrated that this process led to drug amorphization.In vitrodissolution studies showed that all microparticles prolonged MAN release, mainly which one obtained using PCL that contained 5% of drug loaded (PCL-M5). Animal studies demonstrated that formulationPCL-M5was able to keep the variation of mean arterial pressure after phenylephrine administration up to 24 hours. These data confirmed the sustained antihypertensive effect of the investigated microparticles. Results provided an experimental basis for using formulationPCL-M5as a feasible carrier for oral controlled release of MAN intended for treating high blood pressure.


Author(s):  
Subhasri Mohapatra ◽  
Sourabh Jain ◽  
Karunakar Shukla

Memantine hydrochloride is a is a reversible cholinesterase inhibitor used in the treatment of Alzheimer’s disease, low-moderate affinity, uncompetitive n-methyl-d-aspartate (NMDA) receptor antagonist, with strong voltage dependency and rapid blocking/unblocking kinetics. The present study was explore the potential of thermosensitive nanogel of mamentine loaded nanoparticle. In situ gel choosing due to restrict unwanted exposure in blood and other healthy tissues, thus eliminate hemolytic side effects of the drug and offer easy administration in vivo. Nanoparticle prepared by ionic gelation method and further the dried nanoparticle incorporates with in situ gel.  The in situ gel prepared by cold method using the solutions of Poloxamer-188 and Carbopol-934. The Transmission electron microscopy showed the spherical particles  with  smooth surface which was in conformity  with the SEM and Zetasizer  data for particle size. The pH of the formulations was found to be satisfactory and was in the range of 6.8±0.039 -7.4±0.053 and also mucoadhesive strength was show in table. The mucoadhesive strength of all formulations was varies from 2398±0.0004 to 4945±0.0002 dynes/cm2. In-vitro diffusion study of the in situ gel (N1-N8) was performed using modified Franz diffusion cell with dialysis membrane in phosphate buffer pH 6.5 for a period of 24 hours. The in vitro release study were fitted into various kinetic models viz zero order, first order, higuchi model and korsmeyer peppas equation. Stability studies for optimized formulations were carried out at 4.0 ± 0.5°C and 37 ± 0.5ºC for a period of four weeks. There was no significant variation found in physical appearance, average particle size and % drug content of the in situ nanogel N2. No visible changes in the appearance of the gel formulation were observed at the end of the storage period.


INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (04) ◽  
pp. 47-52
Author(s):  
S. C. B Penjuri ◽  
R. Nagaraju ◽  
S. Shaik ◽  
S. Damineni ◽  
S. R. Poreddy ◽  
...  

Gastroretentive dosage forms are useful to extend release of drugs having a narrow window of absorption in the upper intestine and for drugs degraded by higher pH or for drugs with local action in the proximal part of the GI tract. In the present study, an attempt was made to prepare microballoons of riboflavin by emulsion solvent diffusion method by using HPMC and ethylcellulose in order to extend the drug release in the upper GIT, which may result in enhanced absorption and thereby improved bioavailability. The size and surface morphology of riboflavin microballoons were characterized by optical and scanning electron microscopy. FTIR and DSC studies revealed no drug excipient interaction. Average particle size of microballoons was found to be between 126.8±2.26 to 163.4±2.52 μm. Microballoons were found to be spherical in shape with smooth surface texture. Percentage yield of the microballoons was satisfactory. In vitro buoyancy of the optimized riboflavin microballoons was found to be 96.24±0.08%, indicating good floating in stomach. Cumulative amount of drug release from microballoons at the end of 12 hr was 99.78±2.78 % and followed Highuchi diffusion kinetics and super case II transport.


2021 ◽  
Author(s):  
Faten Eshrati Yeganeh ◽  
Amir Eshrati Yeganeh ◽  
Bahareh Farasati Far ◽  
Iman Akbarzadeh ◽  
Sameer Quazi ◽  
...  

Abstract An innovative and customized drug delivery system for in vitro cancer treatment has been developed successfully by a simple one-step method. A CoFe2O4@Methionine core-shell nanoparticle was prepared by the reflux assay, in which amino acid on the surface makes the ferrite biocompatible, enhances the chemical stability of the compound, and increases the drug loading capacity. The synthesized nanoparticles were evaluated using SEM, TEM, FTIR, and VSM, while XRD and TGA analysis verified the presence of a coating amino acid on the surface of CoFe2O4. The appearance of a new peak for C≡N in the FTIR spectrum validates the synthesis of a letrozole-loaded carrier. Both uncoated CoFe2O4 and methionine-coated CoFe2O4 nanoparticles behave super-paramagnetically at room temperature, with saturation values of 46 emu/g and 16.8 emu/g, respectively. SEM and TEM were used to characterize the morphology and size of samples, revealing that the average particle size was around 28–29 nm. The loading of Letrozole and the effect of pH (5, 7.4) on the release behavior of the carrier were studied. The result of the drug release in pH (5) was about 88% higher than pH (7.4). Also, the preparation has been evaluated for determining its cytotoxicity using MCF-7, MDA-MB-231, and MCF10A cell lines as an in vitro model, and the results of in vitro experiments showed that CoFe2O4@Methionine could significantly reduce cancer in the cell model. These results demonstrate that core-shell nanoparticles were prepared that are biocompatible and have potential use as drug delivery.


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