Characterization of Polymeric Micelles for Pulmonary Delivery of Beclomethasone Dipropionate

2006 ◽  
Vol 6 (9) ◽  
pp. 3095-3101 ◽  
Author(s):  
Nazar Noureen Gaber ◽  
Yusrida Darwis ◽  
Kok-Khiang Peh ◽  
Yvonne Tze-Fung Tan
Keyword(s):  
Sustained Release ◽  
Polymeric Micelles ◽  
Pulmonary Delivery ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Chronic Obstructive ◽  
Physical Interaction ◽  
Mass Median Aerodynamic Diameter ◽  
Aerodynamic Diameter ◽  
Mass Median

The potential of using poly-(ethylene oxide)-block-distearoyl phosphatidyl-ethanolamine (mPEG-DSPE) polymer to prepare BDP-loaded micelles with high entrapment efficiency and mass median aerodynamic diameter of less than 5 μm demonstrating sustained release properties was evaluated. The result showed that lyophilized BDP-loaded polymeric micelles with entrapment efficiency of more than 96% could be achieved. Entrapment efficiency was affected by both the drug to polymer molar ratio and the amount of drug used. Investigation using FTIR and DSC confirmed that there was no chemical or physical interaction and the drug was molecularly dispersed within the micelles. TEM images showed that the drug-loaded polymeric micelles were spherical in shape with multivesicular morphology. Further analysis by photon correlation spectroscopy indicated that the particle size of the BDP-loaded micelles was about 22 nm in size. In vitro drug release showed a promising sustained release profile over six days following the Higuchi model. The mass median aerodynamic diameter and fine particle fraction were suitable for pulmonary delivery. Moreover, the small amount of deposited drug in the induction port (throat deposition) suggested possible reduction in incidence of oropharyngeal candidiasis, a side effect normally associated with inhaled corticosteroids therapy. The high encapsulation efficiency, comparable inhalation properties, sustained release behavior together with biocompatibility nature of the polymer support the potential of BDP-loaded polymeric micelles as a versatile delivery system to be used in the treatment of asthma and chronic obstructive pulmonary disease.

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.

Discriminating Ability of Abbreviated Impactor Measurement Approach (AIM) to Detect Changes in Mass Median Aerodynamic Diameter (MMAD) of an Albuterol/Salbutamol pMDI Aerosol

2017 ◽  
Vol 18 (8) ◽  
pp. 3296-3306
Author(s):  
J . David Christopher ◽  
Rajni B. Patel ◽  
Jolyon P. Mitchell ◽  
Terrence P. Tougas ◽  
Adrian P. Goodey ◽  
...  
Keyword(s):  
Mass Median Aerodynamic Diameter ◽  
Aerodynamic Diameter ◽  
Mass Median ◽  
Measurement Approach ◽  
Discriminating Ability

Investigation of the distribution of particles of drugs with the help of cascade impactor

2020 ◽  
pp. 28-33
Author(s):  
D.V. Dobrianskyi ◽  
D.V. Holyshkin ◽  
O.V. Los ◽  
A. Balatskyi ◽  
O. Troshyna
Keyword(s):  
Great Britain ◽  
Standard Deviation ◽  
Respiratory System ◽  
Aerosol Particles ◽  
Cascade Impactor ◽  
Geometric Standard Deviation ◽  
Mass Median Aerodynamic Diameter ◽  
Aerodynamic Diameter ◽  
New Generation ◽  
Mass Median

BACKGROUND. Successful nebulization is a result of joint usage of nebulizer and medication, which equally define availability and disposition of the active substance. Amount of the substance delivered by different nebulizer systems may differ in more than 10 times. OBJECTIVE. The aim of the study was to investigate the distribution of aerosol particles of drugs for inhalation manufactured by «Yuria-Pharm» under conditions of usage of Ulaizer Home. MATERIALS AND METHODS. We investigated Ulaizer Home nebulizer and medications for inhalation (Decasan, Lorde hyal, Nebufluson, Nebutamol) with the help of new generation impactor (“Copley Scientific Limited”, Great Britain). RESULTS AND DISCUSSION. Mass median aerodynamic diameter (MMAD) of Decasan particles was 4.878 µm, geometric standard deviation (GSD) – 1.72. MMAD of Lorde hyal particles was 3.194 µm, GSD – 1.556. Drop distribution for Nebutamol was alike the distribution for non-viscous aqueous solutions (MMAD – 5.363 µm, GSD – 1.924). For Nebufluson MMAD was 5.491 µm, GSD – 1.724. CONCLUSIONS. The delivery of the inhaled drug to the required area of the respiratory system is a key to successful nebulization. It directly depends on the parameters of the aerosol. The distribution of particles of drugs manufactured by «Yuria-Pharm» in case of nebulization using Ulaizer Home allows to deliver the required amount of drug to the predefined parts of the respiratory system.

Effect of nebulized lidocaine on ventilatory response to CO2 in healthy subjects

1993 ◽  
Vol 74 (3) ◽  
pp. 1419-1424 ◽  
Author(s):  
M. J. Mador
Keyword(s):  
Particle Size ◽  
Local Anesthetic ◽  
Healthy Subjects ◽  
Ventilatory Response ◽  
Mass Median Aerodynamic Diameter ◽  
Aerodynamic Diameter ◽  
Control Solution ◽  
Co2 Rebreathing ◽  
Mass Median ◽  
Ventilatory Response To Co2

Partial vagal blockade produced by inhalation of a local anesthetic aerosol has enhanced CO2 responsiveness in some studies but not in others. The effect of inhaled local anesthetic may depend on the amount of drug depositing in the central airways, i.e., the degree of airway anesthesia. We examined the ventilatory response to CO2 rebreathing in 11 healthy subjects before and after inhalation of 4% lidocaine and a normal saline control solution. Lidocaine and control solutions were aerosolized via two different nebulizers: one produced particles with a mass median aerodynamic diameter of 5.28 microns, and the other produced particles with a mass median aerodynamic diameter of 1.76 microns. The ventilatory response to CO2 was not affected by the control solution. In contrast, the ventilatory response to CO2 was significantly increased after aerosolized lidocaine when administered via the moderate-particle-size nebulizer (2.13 +/- 0.66 vs. 1.83 +/- 0.54 l.min-1.Torr-1 during control, P = 0.01) but not via the small-particle-size nebulizer (1.96 +/- 0.82 vs. 1.94 +/- 0.84 l.min-1.Torr-1 during control, P = NS). The increase in ventilation was achieved predominantly by an increase in frequency (P = 0.01) while tidal volume was unchanged. In conclusion, airway receptors accessible to inhaled local anesthetic play a role in the control of breathing during CO2 rebreathing. Previous negative studies may be due to differences in nebulizer technique, affecting the amount of drug depositing within the central airways.

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.

Mannose Conjugated Starch Nanoparticles for Preferential Targeting of Liver Cancer

2020 ◽  
Vol 17 ◽  
Author(s):  
Akhlesh Kumar Jain ◽  
Hitesh Sahu ◽  
Keerti Mishra ◽  
Suresh Thareja
Keyword(s):  
Side Effects ◽  
Liver Cancer ◽  
Entrapment Efficiency ◽  
Xrd Analysis ◽  
In Vitro Cytotoxicity ◽  
Physical Interaction ◽  
Scanning Calorimetry ◽  
Starch Nanoparticles

Aim: To design D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for site specific delivery. Background: Liver cancer is the third leading cause of death in world and fifth most often diagnosed cancer is the major global threat to public health. Treatment of liver cancer with conventional method bears several side effects, thus to undertake these side effects as a formulation challenge, it is necessary to develop novel target specific drug delivery system for the effective and better localization of drug into the proximity of target with restricting the movement of drug in normal tissues. Objective: To optimize and characterize the developed D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for effective treatment of liver cancer. Materials and methods: 5-FU loaded JFSSNPs were prepared and optimized formulation had higher encapsulation efficiency were conjugated with D-Mannose. These formulations were characterized for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning Calorimetry. Potential of NPs were studied using in vitro cytotoxicity assay, in vivo kinetic studies and bio-distribution studies. Result and discussion: 5-Fluorouracil loaded NPs had particle size between 336 to 802nm with drug entrapment efficiency was between 64.2 to 82.3%. In XRD analysis, 5-FU peak was diminished in the diffractogram, which could be attributed to the successful incorporation of drug in amorphous form. DSC study suggests there was no physical interaction between 5- FU and Polymer. NPs showed sustained in vitro 5-FU release up to 2 hours. In vivo, mannose conjugated NPs prolonged the plasma level of 5-FU and assist selective accumulation of 5-FU in the liver (vs other organs spleen, kidney, lungs and heart) compared to unconjugated one and plain drug. Conclusion: In vivo, bio-distribution and plasma profile studies resulted in significantly higher concentration of 5- Fluorouracil liver suggesting that these carriers are efficient, viable, and targeted carrier of 5-FU treatment of liver cancer.

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