Synthesis and SEM Analysis of Ketoprofen-Hidroxipropil-β-Cyclodextrin Microparticles for Medical Applications as Drug-Release System with a High Bioavailability

2013 ◽  
Vol 325-326 ◽  
pp. 106-110
Author(s):  
Monica Stamate Cretan ◽  
Corneliu Munteanu ◽  
Eliza Gafitanu ◽  
Andreea Carmen Barbinta ◽  
Ciprian Stamate

Drug-release systems are studied lately for increasing absorption in the body and improve the therapeutic effectiveness is key objective. Whatever form it may take a drug release system: tablet, implant, injectable suspension or transdermal system, the basic unit on which effective therapeutic drug particle. Knowledge of particle size distribution in a disperse system is of great importance in pharmaceutical technology. The size, surface area and volume-surface particle may be relevant to the physical, chemical and pharmacological drug toxicities. Stability and speed of dissolution of ketoprofen are much reduced in pure and coupled with a solubility promoter, enhances the bioavailability and particle size distribution depends. In order to improve absorption properties of ketoprofen were synthesized drug microparticles containing ketoprofen and hydroxypropyl beta cyclodextrin. Drug microparticles were studied by SEM microscopy and the results correlated with solubility properties. It was found that microparticles obtained are more easily soluble than pure ketoprofen and small size increases bioavailability.

Author(s):  
Faisalina Ahmad Fisol ◽  
Fabio Sonvico ◽  
Paolo Colombo ◽  
Amirul Al-Ashraf Abdullah ◽  
Habibah A. Wahab ◽  
...  

Polyhydroxyalkanoate (PHA) co-polymers show relatively higher in vivo degradation rate compared to other PHAs thus they received a great deal of attention for a wide range of medical applications. Nanoparticles (NPs) loaded with poorly water soluble anticancer drug docetaxel (DCX) were produced using poly 3-hydroxybutyrate-co-4-hydroxybutyrate, P(3HB-co-4HB), co-polymers biosynthesised from Cupriavidus sp. USMAA1020 isolated from Malaysian environment. Three co-polymers with different molar proportions of 4-hydroxybutirate (4HB) were used: 16% (PHB16), 30% (PHB30) and 70% (PHB70) 4HB-containing P(3HB-co-4HB). Blank and DCX loaded nanoparticles were then characterized for their size and size distribution, surface charge, encapsulation efficiency and drug release. Pre-formulation studies showed that an optimised formulation could be achieved through the emulsification/solvent evaporation method using PHB70 with the addition of 1.0% PVA, as stabilizer and 0.03% VitE-TPGS, as surfactant. DCX-loaded PHB70 nanoparticles (DCX-PHB70) gave the desired particle size distribution in term of average particles sizes around 150 nm and narrow particle size distribution (PDI below 0.100). The encapsulation efficiencies result showed that at 30% w/w drug-to-polymer ratio: DCX- PHB16 NPs were able to encapsulate up to 42% of DCX; DCX-PHB30 NPs encapsulated up to 46% of DCX and DCX-PHB70 NPs encapsulated up to 50% of DCX within the nanoparticles system. Approximately 60% of DCX was released from the DCX-PHB70 NPs within 7 days for 5%, 10% and 20% of drug to polymer ratio while for the 30% and 40% drug to polymer ratios, an almost complete drug release (98%) after 7 days of incubation was observed.


Author(s):  
Matthew Lam ◽  
Ali Nokhodchi

Abstract Purpose Liqui-Tablet is a dosage form derived from Liqui-Mass technology. It has proven to be a promising approach to improve drug dissolution rate of poorly water-soluble drugs. So far, Liqui-Tablet is feasible for low-dose drugs. In this study, an attempt was made to produce high-dose Liqui-Tablet, whilst maintaining ideal physicochemical properties for ease of manufacturing. Methods Liqui-Tablets containing 100 mg of ketoprofen were produced using various liquid vehicles including PEG 200, Span 80, Kolliphor EL, PG, and Tween 85. Investigations that were carried out included saturation solubility test, dissolution test, tomographic study, and typical quality control tests for assessing flowability, particle size distribution, friability, and tablet hardness. Results The weight of these Liqui-Tablets was acceptable for swallowing (483.8 mg), and the saturation solubility test showed PEG 200 to be the most suitable liquid vehicle (493 mg/mL). Tests investigating physicochemical properties such as flowability, particle size distribution, friability, and tablet hardness have shown no issue concerning quality control and manufacturability. The drug release test of the best formulation has shown extremely rapid drug release at pH 7.4 (100% after 5 min). At pH 1.2 the drug release was reasonable considering the formulation was yet to be optimized. Conclusion Despite the high amount of API and liquid vehicle, it is possible to produce a high-dose dosage form with acceptable size and weight for swallowing using the novel Liqui-Mass technology. This has the potential to diversify the technology by removing the restriction of high dose drug that has been seen in liquisolid technology.


Nanomaterials ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 2123 ◽  
Author(s):  
A.F. Faisalina ◽  
Fabio Sonvico ◽  
Paolo Colombo ◽  
A.A. Amirul ◽  
H.A. Wahab ◽  
...  

Polyhydroxyalkanoate (PHA) copolymers show a relatively higher in vivo degradation rate compared to other PHAs, thus, they receive a great deal of attention for a wide range of medical applications. Nanoparticles (NPs) loaded with poorly water-soluble anticancer drug docetaxel (DCX) were produced using poly(3-hydroxybutyrate-co-4-hydroxybutyrate), P(3HB-co-4HB), copolymers biosynthesised from Cupriavidus malaysiensis USMAA1020 isolated from the Malaysian environment. Three copolymers with different molar proportions of 4-hydroxybutirate (4HB) were used: 16% (PHB16), 30% (PHB30) and 70% (PHB70) 4HB-containing P(3HB-co-4HB). Blank and DCX-loaded nanoparticles were then characterized for their size and size distribution, surface charge, encapsulation efficiency and drug release. Preformulation studies showed that an optimised formulation could be achieved through the emulsification/solvent evaporation method using PHB70 with the addition of 1.0% PVA, as stabilizer and 0.03% VitE-TPGS, as surfactant. DCX-loaded PHB70 nanoparticles (DCX-PHB70) gave the desired particle size distribution in terms of average particle size around 150 nm and narrow particle size distribution (polydispersity index (PDI) below 0.100). The encapsulation efficiency result showed that at 30% w/w drug-to-polymer ratio: DCX- PHB16 NPs were able to encapsulate up to 42% of DCX; DCX-PHB30 NPs encapsulated up to 46% of DCX and DCX-PHB70 NPs encapsulated up to 50% of DCX within the nanoparticle system. Approximately 60% of DCX was released from the DCX-PHB70 NPs within 7 days for 5%, 10% and 20% of drug-to-polymer ratio while for the 30% and 40% drug-to-polymer ratios, an almost complete drug release (98%) after 7 days of incubation was observed.


MRS Bulletin ◽  
1997 ◽  
Vol 22 (12) ◽  
pp. 19-23 ◽  
Author(s):  
Dennis R. Dinger ◽  
James E. Funk

Particle packing is directly controlled by the particle-size distribution of a material being processed. For this reason, particle packing is important to all particulate/fluid systems. After the solids fraction of a body is defined, interparticle chemistry controls how the body will pack and flow. A system of powders can never pack better than the maximum possible level defined by the particle-size distribution alone. Proper control of interparticle chemistry however can help achieve maximum packing, can be used to open the structure, and/or can be used to modify rheological or other process properties.The main goals of particle-packing research have been to determine how systems of particles pack, to develop algorithms for calculating packing densities and porosities for any distribution of particles (spherical or nonspherical, rough or smooth, wet or dry), and to determine how packing and its properties affect the variety of industrial operations that utilize particulate/fluid systems.


Folia Medica ◽  
2021 ◽  
Vol 63 (1) ◽  
pp. 97-104
Author(s):  
Amit Bansal ◽  
Brian Krieg ◽  
Navneet Sharma ◽  
James McGinnis ◽  
Inderdeep Bhatia ◽  
...  

Introduction: Bitter tasting of drugs leads to non-compliance especially in the case of pediatric patients due to their inability to swal-low medication.  Aim: In this study, we aimed to mask the bitter taste of acetaminophen (APAP) particles through coating.  Materials and methods: A pH independent water insoluble ethylcellulose polymer was used to coat the APAP. The coating of water insoluble ethylcellulose on APAP can have a significant impact on the dissolution profile. Various grades of APAP were used for coating; fine grade, Compap L90% having wide particle size distribution (PSD), and a special granular (SG) APAP 1680 having narrow PSD. Coating was performed using top spray (Vector) for Compap L90% and SG APAP 1680 grade of APAP.  Results: Bitter taste of SG APAP was masked after spraying dispersion equivalent to a weight gain of 10% compared to 35% used for Compap L90%. Using bottom spray (Wurster coater, GPCP 2.0), coating was performed on SG APAP 1680 grade of APAP by spraying aqueous dispersion of ethylcellulose (Surelease) equivalent to a weight gain of 10%. The scalability of the top spray process was also evaluated in GPCG 30 and bitter taste was masked by using Surelease dispersion equivalent to a weight gain of 6%. Coated APAP was examined for particle size (PS), particle size distribution (PSD), flowability, and drug release profile. Dissolution was performed using USP apparatus 2 and 4 in phosphate buffer and evaluated for mechanism of drug release. Particle size obtained for coated SG APAP 1680 via top and bottom spray process was 404 µm d(90) and 487 µm d(90) respectively.  Conclusions: The results of the study demonstrated the potential of Surelease dispersion in taste masking. The use of SG APAP 1680 having narrow PSD allowed taste masking to achieve at low weight gain without greatly affecting the dissolution profile.


2020 ◽  
Vol 33 (7) ◽  
pp. 1126-1137
Author(s):  
Edwin Peter Chang'a ◽  
Medani Eldow Abdallh ◽  
Emmanuel Uchenna Ahiwe ◽  
Said Mbaga ◽  
Ze Yuan Zhu ◽  
...  

Objective: Pellet durability, particle size distribution, growth response, tibia bone characteristics and energy retention were measured to evaluate cassava as an alternative energy source to replace maize in broiler diets with or without Ronozyme (A+VP) enzyme composites.Methods: A total of 480 one-day broiler chicks were randomly assigned to 8 treatments in a 4×2 factorial arrangement. Four levels of cassava: (0%, 25%, 50%, 75%) and 2 levels of enzymes (0 and 500 g/tonne) were used. Each treatment was replicated six times, with ten birds per replicate.Results: The particle size distribution in the diets showed an increasing trend of small particles with increase in cassava level. Pellet durability decreased (p<0.05) with cassava inclusion. Feed intake was highest in birds fed diets with medium cassava level at 1 to 24 d and 1 to 35 d of age. The body weight gain of birds reduced (p<0.037) as cassava level increased, but it increased (p<0.017 when enzymes were added. The feed conversion ratio was high (p<0.05) when cassava level was increased, but it reduced (p<0.05) when enzymes were added. The dressing percentage (DP), and weight of drumsticks reduced (p<0.05) with increasing cassava level. Enzyme supplementation increased (p<0.05) DP, and weight of breast, thighs and drumsticks. Ash content, weight, length, width, and bone strength decreased (p<0.05) when cassava level was increased, however, they were increased with enzyme addition. The contents of Ca, K, and Zn were raised (p<0.001) with increasing cassava level. Enzyme inclusion increased (p<0.001) all mineral contents in tibia bones. Body fat and energy retained as fat decreased (p<0.001) as cassava level increased. Enzyme inclusion increased (p<0.05) body protein content and energy retained as protein.Conclusion: Although broiler performance was depressed by high levels of cassava inclusion, it was not affected by low levels, which further improved by enzyme supplementation.


Author(s):  
Mohamad Rais Hasan ◽  
Mohd Sabri Mohd Ghazali ◽  
Nor Fazliyana Mohtar

Hydroxyapatite (HAp) with the chemical formula of Ca10(PO4)6(OH)2is a mineral component found in bone structure, and has broad application in many fields. Several sources can be used for the extraction of HAp either synthetic or natural. However, sources such as porcine and bovine have drawbacks that decreased the demand of HAp. This study aimed to extract and determine particle size distribution and pore characteristics of hydroxyapatite nanoparticles (HAp NPs) derived from spotted sardinella (Amblygaster sirm). Further characterization of extracted HAp NPs was carried out by Scanning Electron Microscopy (SEM), Energy Dispersive X-ray Spectroscopy (EDS) and Brunauer–Emmett–Teller(BET). SEM analysis has shown that the extracted HApNPs has an irregularsp here-like shape with particle size distribution ranged from 95nm to 100nm.


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