scholarly journals Design and Characterization of Double Layered Mucoadhesive System Containing Bisphosphonate Derivative

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Dhrubojyoti Mukherjee ◽  
Srinivasan Bharath

The objective of this study is to evaluate the effect of formulation variables on different evaluation properties such as cumulative percentage release and swelling index in development of two layered buccal mucoadhesive system consisting of a highly water soluble drug risedronate sodium. The mucoadhesive systems were developed with varied concentrations of the polymers (1-2%) using plasticizer/permeation enhancer (25–50% w/w of polymer). Two layered films comprised of risedronate sodium with chitosan (85% deacetylated) and hydroxypropylmethyl cellulose (HPMC 4KM) interpolymer complex of different ratios were prepared by solvent casting method. An impermeable backing membrane of ethyl cellulose was incorporated into the films. The study shows the effect of multipolymeric films on the release of a bisphosphonates derivative. The optimized formulations showed films with uniform drug content (90.91±0.17–105.53%±2.15), thickness (0.22±0.01 mm to 0.31±0.06 mm), mucoadhesivity (26±3.61–42.33±2.82 g), and controlled drug release profile up to a period of 10 hours. The films were also studied for swelling index, moisture uptake, viscosity, folding endurance, water vapor transmission rate, and mucoadhesive time.

Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.


2019 ◽  
Vol 16 (5) ◽  
pp. 1351-1365
Author(s):  
Muhammad Iqbal Nasiri ◽  
Rabia Ismail Yousuf ◽  
Muhammad Harris Shoaib ◽  
Kamran Zaheer ◽  
Tariq Ali ◽  
...  

Author(s):  
Deepak Patil ◽  
Seema Pattewar ◽  
Sarvesh Palival ◽  
Gargi Patil ◽  
Swapnil Sharma

The aim of present study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of quetiapine fumarate, a second-generation antipsychotic drug. Quetiapine Fumarate (QF) loaded NLC were prepared by hot homogenization followed by an ultrasonication method. Response surface methodology - central composite design (CCD) was used to systemically examine the influence of concentration of capmul MCM EP, concentration of poloxamer 188 and concentration of egg lecithin on particle size (PS) and % entrapment efficiency (% EE) and to optimize the NLC formulation. The CCD consists of three factored design with five levels, plus and minus alpha (axial points), plus and minus 1 (factorial points) and the centre point. A mathematical relationship between variables was created by using Design Expert software Version 12. The statistical evaluations revealed that three independent variables were the important factors that affected the PS and % EE of QF loaded NLC. The best fitted mathematical model was linear and quadratic for PS and % EE respectively. The optimized formulations found with 218.1±0.14nm of PS and 93±0.16% of % EE. Results illustrated the superiority of developed QF loaded NLC formulation as a stable drug delivery system, providing better bioavailability with the possibility of better treatment for psychological disorders.


2009 ◽  
Vol 59 (4) ◽  
pp. 453-461 ◽  
Author(s):  
Vikrant Vyas ◽  
Pankajkumar Sancheti ◽  
Poonam Karekar ◽  
Manali Shah ◽  
Yogesh Pore

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407 Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (DE30 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characteristics of the polymer at its higher concentration, which might have retarded the release rate of tadalafil.


1970 ◽  
Vol 7 (2) ◽  
pp. 127-132 ◽  
Author(s):  
Bendgude Namdeo ◽  
Iyer Vidya ◽  
Poddar Sushilkumar

In the present investigation an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by developing controlled release matrix tablets of diltiazem hydrochloride. Diltiazem hydrochloride was formulated as oral controlled release matrix tablets by using sterculia foetida gum. SFG fines were characterized with scanning electron microscopy. The purpose of this study was to optimize release profile of the highly water soluble drug from SFG matrix by using water soluble and swellable excipients like lactose and microcrystalline cellulose respectively. Tablets were prepared by direct compression, and their swelling behavior in presence of these excipients was assessed with the help of a Texture Analyzer. Dissolution assessment was performed using USP 26 apparatus 2 modified by insertion of a mesh to prevent sticking of the tablets to the bottom of vessel and allow them to swell three dimensionally. The interdependence of swelling front movement in relation to excipients type and progression of drug release are explained. It was concluded that unlike in conventional dosage forms insertion of excipients in hydrophilic controlled release tablets containing a water soluble drug gave the finger print information of drug release profile. In vitro drug release from these matrices was characterized and confirmed with the help of real time texture probing. Results indicated that it is possible to achieve desired modulation in the drug release profile by inclusion of lactose and microcrystalline cellulose. Key words: Diltiazem HCl, Sterculia Foetida Gum, Swelling and erosion, Lactose, Texture analysis. doi: 10.3329/dujps.v7i2.2167 Dhaka Univ. J. Pharm. Sci. 7(2): 127-132, 2008 (December)


2015 ◽  
Vol 51 (3) ◽  
pp. 663-671 ◽  
Author(s):  
Vikas Bhandari ◽  
Amelia Avachat

The purpose of present study was aimed at developing self emulsifying drug delivery system in liquid and then in pellet form that would result in improved solubility, dissolution and permeability of the poorly water soluble drug carvedilol. Pellets were prepared using extrusion-spheronization technique incorporating liquid SEDDS (carvedilol, capmul MCM EP, cremophore EL, tween 20, propylene glycol), adsorbents ( and crospovidone), microcrystalline cellulose and binder (povidone K-30). Ternary phase diagram was constructed to identify different oil-surfactant-cosurfactant mixtures according to the proportion of each point in it. The optimal CAR-SEDDS pellets showed a quicker redispersion with a droplet size of the reconstituted microemulsion being 160.47 nm, which was almost unchanged after solidification. SEM analysis confirmed good spherical appearance of solid pellets; DSC and XRD analysis confirmed that there was no crystalline carvedilol in the pellets. Pellets were then capable of transferring lipophilic compounds into the aqueous phase and significantly enhancing its release with respect to pure drug.


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