scholarly journals NANO-VESICLES OF SALBUTAMOL SULPHATE IN METERED DOSE INHALERS: FORMULATION, CHARACTERIZATION AND IN VITRO EVALUATION

2017 ◽  
Vol 9 (6) ◽  
pp. 100 ◽  
Author(s):  
Mona G. Arafa ◽  
Bassam M. Ayoub
Keyword(s):  
In Vitro Release ◽  
Pulmonary Delivery ◽  
Entrapment Efficiency ◽  
Reversed Phase ◽  
Molar Ratio ◽  
Metered Dose Inhalers ◽  
Salbutamol Sulphate ◽  
Novel Approach ◽  
Metered Dose

Objective: The present work was aimed to prepare niosomes entrapping salbutamol sulphate (SS) using reversed phase evaporation method (REV).Methods: Niosomes were prepared by mixing span 60 and cholesterol in 1:1 molar ratio in chloroform, SS in water was then added to organic phase to form niosomal SS. Formulations after evaporation of chloroform, freeze centrifuged then lyophilized, were evaluated for particles size, polydispersity index (Pdi), zeta-potential, morphology, entrapment efficiency (EE%) and in vitro release. For pulmonary delivery; metered dose inhalers (MDI) were prepared by suspending SS niosomes equivalent to 20 mg SS in hydrofluoroalkane (HFA). The metered valve was investigated for leakage rate, the total number of puffs/canister, weight/puff, dose uniformity and particle size.Results: The results showed spherical niosomes with 400-451 nm particles that entrapped 66.19% of SS. 76.54±0.132% SS release from niosomes that showed a controlled release profile for 8h. The leakage test was not exceeding 4 mg/3 d, the number of puffs were up to 200puffs/canister, the dose delivered/puff was 0.1 mg and 0.64-4.51μm niosomal aerosol.Conclusion: The results indicate an encouraging strategy to formulate a controlled drug delivery by entrapping (SS) in niosomes which could be packaged into (MDI) that met the requirements of (USP) aerosols guidelines which offering a novel approach to respiratory delivery.

Formulation and Evaluation of Nanosponges loaded Bifonazole for Fun-gal Infection

2020 ◽  
Vol 18 ◽  
Author(s):  
Amaravathi Murali Krishna ◽  
Venkatesh Dinnekere Putte Gowda ◽  
Roopa Karki
Keyword(s):  
Drug Release ◽  
Fungal Infections ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Three Dimensional ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Model Stability ◽  
Novel Approach

Background: Nanosponges is a novel approach of topical drug delivery, especially for the fungal infections. Nanosponges are a unique class of nanoparticles with three-dimensional nanostructure in nanometers wide cavities, which can encapsulate both hydrophilic and lipophilic substances, will provide increased efficacy and safety. Objective: To formulate and evaluate Bifonazole loaded nanosponges in hydrogels for the treatment of fungal diseases. Methods: Bifonazole-loaded nanosponges to be formulated using emulsion solvent diffusion technique. Interaction of drugethyl cellulose polymer along with other excipients’ was done by using FTIR as well as DSC. The nanosponges formulations were evaluated with different parameters. Results: Bifonazole loaded nanosponges’ particle size and zeta potential for formulations were between the range of 183.7 to 560.2 nm and –17.77 to –21.9 mV, respectively. Surface morphology of nanosponges by SEM disclosed that it was spherical and porous in nature. Drug entrapment efficiency was found to be 45.44 to 79.71%. The drug release study was done by using phosphate buffer pH 6.8. Further in vitro release data is fitted in to kinetic models. The optimized formulation M6 has incorporated hydrogels, further evaluated skin irritation, in vitro drug release, viscosity and pH using a rat model. Stability studies of hydrogel formulation MH2 revealed that no changes in in-vitro drug release, pH and drug content study at the completion of 6 months. Conclusion: Thus, it indicated that the prepared Bifonazole loaded nanosponges into hydrogel was stable. Hence, it could be a suitable dosage form for the cure of fungal infections in the skin.

Elastic Bilayer Vesicles of Flurbiprofen for Transdermal Delivery: Development and In-Vitro Characterization

2020 ◽  
Vol 10 (1) ◽  
pp. 54-60
Author(s):  
Rashmi Sareen ◽  
Nitin Jain
Keyword(s):  
Transdermal Delivery ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Systemic Circulation ◽  
Molar Ratio ◽  
Vesicle Size ◽  
Cholesterol Ratio ◽  
Niosomal Gel ◽  
Span 60

Objective: The purpose of the present study was to develop a novel elastic bilayer vesicle entrapped with Flurbiprofen (FLB) for transdermal use to avoid adverse effect associated with oral administration of the drug. Encapsulation of drug in vesicle prolongs the existence of the drug in the systemic circulation and thus enhances penetration into the target site and reduces toxicity. Method: Niosomes were prepared using surfactants (span 40 and span 60) and cholesterol in the molar ratio of 1:1, 2:1, 3:1 and 3:2. Vesicles prepared by thin film hydration method were characterized for morphology, vesicle size and zeta potential, thermal analysis and Entrapment Efficiency (EE). Results: Results revealed that the EE and size of niosomes were influenced by surfactant type and cholesterol ratio. F8 (span 60: cholesterol in 3:2) exhibited the highest encapsulation of FLB (76.77 ± 0.55) with vesicle size of 154 ± 2.96 nm and Polydispersity Index (PDI) of 0.09. The optimized formulation F8 was selected for incorporation into the gel. Niosomal gel was evaluated for homogeneity, pH, spreadability and in-vitro drug release. Conclusion: All the parameters of niosomal gel were found to be satisfactory and in-vitro release study revealed prolonged and complete release of entrapped FLB (93.23±0.65%) in comparison to FLB hydrogel (42.65±0.29%). The results suggested that niosomes may serve as promising vehicles for the transdermal delivery of FLB.

scholarly journals MANNOSYLATED MULTIWALLED CARBON NANOTUBES ASSISTED ARTESUNATE DELIVERY FOR CEREBRAL MALARIA

2019 ◽  
pp. 24-30
Author(s):  
Anamika Sahu Gulbake ◽  
Aviral Jain ◽  
Satish Shilpi ◽  
Pramod Kumar ◽  
ARVIND GULBAKE
Keyword(s):  
Carbon Nanotubes ◽  
Cerebral Malaria ◽  
Equilibrium Dialysis ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Multiwalled Carbon ◽  
Albino Rat ◽  
Distribution Study ◽  
Novel Approach

Objective: The present investigation focused on the novel approach using artesunate (AS) loaded mannosylated conjugated multi-walled carbon nanotubes (M-MWCNTs) for site-specific delivery to the brain in the treatment of cerebral malaria (CM). Methods: The raw MWCNTs were purified by selective oxidation method and then exposed to sequential chemical functionalization according to the following steps: carboxylation, acylation, amine modification and finally, D-mannose conjugation. The AS was loaded via the equilibrium dialysis method in the molar ratio 1:3 of various functionalized sonicated MWCNTs. The functionalized MWCNTs were characterized for elemental analysis, FTIR, TEM, zeta potential and percentage drug entrapment efficiency. The in vitro drug release study was performed on AS conjugated purified MWCNTs (AS-P-MWCNT) and AS conjugated M-MWCNTs. Bio-distribution study was performed on albino rat for quantitative measurement of AS in different organs and blood. Results: The TEM images of M-MWCNTs indicated their open tubular nature and AS-M-MWCNTs suggests the entrapment of AS. The percent drug entrapment of AS-M-MWCNT was found to be 80.29±3.4 %. In vitro AS release from AS-M-MWCNTs was found in a controlled manner at pH 7.4. The bio-distribution studies clearly indicate the superiority of the AS-M-MWCNTs, as compared to the plain drug towards increasing the accumulation of AS in brain. Conclusion: The results suggest that AS-M-MWCNTs could be employed as an efficient nano-carrier for antimalarial therapy in cerebral malaria.

scholarly journals Synthesis and evaluation of B-cyclodextrin Based Nanosponges of 5- Fluorouracil by Using Ultrasound Assisted Method

2020 ◽  
Vol 29 (2) ◽  
pp. 88-98
Author(s):  
Ihsan K. Jasim ◽  
Shaimaa N. Abd Alhammid ◽  
Alaa A. Abdulrasool
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Particle Morphology ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Phase Solubility ◽  
Molar Ratios ◽  
Phase Solubility Study ◽  
Ultrasound Assisted

  CD-nanosponges were prepared by crosslinking B-CD with diphenylcarbonate (DPC) using ultrasound assisted technique. 5-FU was incorporated with NS by freeze drying, and the phase solubility study, complexation efficiency (CE) entrapment efficiency were performed. Also, the particle morphology was studied using SEM and AFM. The in-vitro release of 5-FU from the prepared nanosponges was carried out in 0.1N HCl. 5-FU nanosponges particle size was in the nano size. The optimum formula showed a particle size of (405.46±30) nm, with a polydispersity index (PDI) (0.328±0.002) and a negative zeta potential (-18.75±1.8). Also the drug entrapment efficiency varied with the CD: DPC molar ratio from 15.6 % to 30%. The SEM and AFM showed crystalline and porous nature of the nanosponges. The in vitro drug release study of the selected formula 5-FUNS2 exhibited the fastest dissolution rate which is 56% in the first hr. Different molar ratios of (cyclodextrin to crosslinker) (CD: DPC) has a proficient effect on complexation efficiency (CE), apparent stability constant (Kst) and entrapment efficiency of 5-FU. 5-FUNS2 with (1:4) molar ratio showed the best result of CE, Kst and entrapment efficiency. 5-FUNS2 gave a higher release rate than the 5-FU-BCD inclusion complex and 5-FU solution. Surface morphology of the prepared nanosponges by SEM, AFM indicate that nanosized and highly porous nanosponges was obtained. The overall results suggest that cyclodextrin nanosponges could be a promising 5-FU delivery system utilizing the suitable formula.

Preparation and In-vitro Evaluation of Fe3O4 Encapsulated by Chitosan Loaded Capecitabine Nanoparticles for the Treatment of Breast Cancer

2016 ◽  
Vol 6 (3) ◽  
Author(s):  
Shanmuganathan S. ◽  
Nigma S. ◽  
Anbarasan B. ◽  
Harika B.
Keyword(s):  
Fe3o4 Nanoparticles ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Evaluation ◽  
Sem Image ◽  
Therapeutic Molecules ◽  
Dialysis Method ◽  
Vitro Release

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.

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.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

scholarly journals Development and Evaluation of Rifampicin Loaded Alginate–Gelatin Biocomposite Microfibers

Polymers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1514
Author(s):  
Ameya Sharma ◽  
Vivek Puri ◽  
Pradeep Kumar ◽  
Inderbir Singh ◽  
Kampanart Huanbutta
Keyword(s):  
Wound Healing ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Entrapment Efficiency ◽  
Tissue Proliferation ◽  
Naturally Occurring ◽  
Reinforcing Material ◽  
Vitro Release

Various systematic phases such as inflammation, tissue proliferation, and phases of remodeling characterize the process of wound healing. The natural matrix system is suggested to maintain and escalate these phases, and for that, microfibers were fabricated employing naturally occurring polymers (biopolymers) such as sodium alginate, gelatin and xanthan gum, and reinforcing material such as nanoclay was selected. The fabrication of fibers was executed with the aid of extrusion-gelation method. Rifampicin, an antibiotic, has been incorporated into a biopolymeric solution. RF1, RF2, RF3, RF4 and RF5 were coded as various formulation batches of microfibers. The microfibers were further characterized by different techniques such as SEM, DSC, XRD, and FTIR. Mechanical properties and physical evaluations such as entrapment efficiency, water uptake and in vitro release were also carried out to explain the comparative understanding of the formulation developed. The antimicrobial activity and whole blood clotting of fabricated fibers were additionally executed, hence they showed significant results, having excellent antimicrobial properties; they could be prominent carriers for wound healing applications.

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