Formulation and Evaluation of Chitosan-Polyaniline Nanocomposites for Controlled Release of Anticancer Drug Doxorubicin

Author(s):  
Dillip Kumar Behera ◽  
Kampal Mishra ◽  
Padmolochan Nayak

In this present work, chitosan (CS) crosslink with polyaniline (PANI) with montmorilonite (MMT) called as (CSPANI/MMT) and CS crosslink with PANI without MMT called as (CS-PANI) were prepared by employing the solution casting method. Further the formation of nanocomposites CS-PANI/MMT and CS-PANI were investigated using XRD, FTIR, SEM and tensile strength. Water uptake and swelling ratio of the CS-PANI and CS-PANI/MMT were found to decrease with increase in concentration of clay. Mechanical properties of the CS-PANI and CS-PANI/MMT were assessed in terms of tensile strength and extensibility using texture analyzer. Increase in tensile strength and reduction in extensibility was reported with increase in the nanoclay content. In vitro drug release study on CS-PANI and CS-PANI/MMT indicated pronounced sustained release of doxorubicin by the incorporation of clay particles in the CS polymer matrix. Overall CSPANI/MMT nanocomposite films exhibited improved mechanical and sustained drug release properties than CS-PANI.

Author(s):  
DILLIP KUMAR BEHERA ◽  
KAMPAL MISHRA

Objective: The purpose of the present study was a characterization of chitosan (CS)-polypyrrole (PPY) nanocomposites for controlled release of anticancer drug doxorubicin (DOX). Methods: Chitosan crosslink with PPY with montmorillonite (MMT) called as (CS-PPY/MMT) were formulated using the solvent casting method. The prepared nanocomposites were characterized by X-Ray Diffraction Analysis (XRD), tensile strength, scanning electronic microscope (SEM). Results: The XRD result confirmed that the CS-PPY/MMT possessed crystal structure. The nanocomposites CS-PPY/MMT-4 were showed a homogenous morphology. The Water uptake and swelling ratio of the CS-PPY and CS-PPY/MMT were found to decrease with increase in the concentration of clay. Mechanical properties of the CS-PPY and CS-PPY/MMT were assessed in terms of tensile strength and extensibility using texture analyzer. Increase in tensile strength and reduction in extensibility was reported with an increase in the nanoclay content. In vitro drug release study on CS-PPY and CS-PPY/MMT indicated pronounced sustained release of doxorubicin by the incorporation of clay particles in CS-PPY/MMT. It was observed that during the first 60 min of the dissolution study, the CS-PPY/MMT-4 film showed just 79.32±0.56% drug release as while the CS-PPY-1, CS-PPY/MMT-2 and CS-PPY/MMT-3 films showed a release of 53.79±1.23%, 63.51±1.24% and 68.15±2.38% respectively. Conclusion: CS-PPY/MMT nanocomposite films exhibited improved mechanical and sustained drug release properties than CS-PPY. The combination of biodegradable polymeric chains and clay reinforcement can be applied to achieve the desired combination of properties of materials used as a biosensor for diverse biomedical applications.


Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.


2017 ◽  
Vol 9 (6) ◽  
pp. 85
Author(s):  
G. Ravi ◽  
N. Vishal Gupta

Objective: The objective of present investigation was to develop rivastigmine tartrate transdermal film employing factorial design.Methods: The formulations were designed by Design-Expert software-version10. A series of films were prepared by solvent casting method using polymers, plasticizer, permeation enhancer and other solvents. Transdermal films were evaluated for flatness, drug content, tensile strength, in vitro drug release and ex vivo skin permeation study.Results: The flatness was found 100% (percentage) for all film formulations. The drug content of transdermal film was found in the range of 96.51±0.2 to 98.81±0.3%. The tensile strength of transdermal film was found in the range of 6.28±0.06 to 11.56±0.03 N/mm2 (newton/millimeter2) and in vitro drug release at 24th h (hour) was found in the range of 86.24±0.25 to 96.1±0.48%% for various formulations and ex vivo skin permeation study results at 24th h was found in the range of 85.83±0.74 to 97.36±0.93%.Conclusion: These results support the feasibility of developing transdermal film of rivastigmine tartrate for human applications. Thus, transdermal delivery of rivastigmine tartrate film is a safe, painless and cost effective drug delivery system for Alzheimer’s patients.


2021 ◽  
Vol 11 (2-S) ◽  
pp. 76-81
Author(s):  
Jddtadmin Journal

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.   Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.


2018 ◽  
Vol 9 (4) ◽  
pp. 107
Author(s):  
R Poonguzhali ◽  
S Khaleel Basha ◽  
V Sugantha Kumari

<p>In this study Ampicillin drug loaded with alginate and nanocellulose film was prepared by solution casting method. Nanocellulose and ampicillin incorporated into alginate to improve both mechanical and swelling property. The formulated ampicillin loaded Alg/NC film gave acceptable physicochemical properties compared with Alg-amp film and was able to deliver the drug in a prolonged release pattern. <em>In vitro</em> drug release showed that alginate, could provide an immediate release of ampicillin with further enhanced nanocellulose, and followed by a sustained release over 500 min of the remaining drug. The present study exhibited a simple and useful approach to systematically design for providing drug release profiles.</p>


2017 ◽  
Vol 5 (02) ◽  
pp. 24-28
Author(s):  
B. Kumar ◽  
G. Jeyabalan

Metformin/Gliclazide niosomes were formulated with span 60 by ether injection method. Three batches MG1-MG3 were prepared in order to study influence of drug polymer ratio on the niosomes formation and in vitro drug release. The formulated niosomes were characterized by drug entrapment, vesicle size determination, and in vitro drug release. Optimized concentration of span 60 and cholesterol was found to be 1:1. In the in-vitro study, niosomes formulation of MG1 showed high percentage of drug release, 40.18 to 45.75% for about 8 hrs. This indicated that this batch of niosomes formulation exhibit sustained drug release pattern as the niosomes act as reservoir system for continuous delivery of drug. The quantity of Metformin/Gliclazide present in the niosomes and the release medium were estimated by a validated HPLC method. The formulated niosomes had acceptable physicochemical characters and released the drug over 6-8 h. The data obtained from in vitro release studies were fitted with various kinetic models and was found to follow Higuchi kinetics.


Author(s):  
Meesala. Srinivasa Rao ◽  
M. S Chandra Goud ◽  
C. V. Reddy

Meloxicam has short biological half-life and is rapidly eliminated, frequent oral administration is necessary to maintain its therapeutic concentration, but this can increase chances of missing dose. This makes Meloxicam a good applicant for oral sustained release formulation. The objective of study was to develop in-situ gel formulations of Meloxicam for sustained release to reduce the dosing frequency in the treatment of rheumatoid arthritis. Method of Ion sensitive in-situ gelation was used in this study. Meloxicam In-situ gel formulations were prepared by varying concentrations of sodium alginate as a bio-degradable gel forming polymer, CaCl2 as a cross-linking agent and Chitosan/ HPMCK4/HPMCK15/Guar gum/Gellan gum/ Xantha gum/pectin were used as drug release rate controlling polymers. The formulations F11-F18 were assessed for Physical appearance, pH, in-vitro drug release, viscosity, in-vitro gelling capacity and drug content. FTIR, DSC and in-vivo drug kinetics studies was conducted for Meloxicam, excipients used and optimized formulation. Formulations showed an optimum viscosity that will allow ease of administration and swallowing. All formulations are shown pH between4.7-4.9, floating lag time was 2-3sec and floated for >12 hrs. In vitro drug release studies reporting that commercially available product Meloxicam SR has showed 99.92% drug release in 8 hrs and out of eight formulations F11 showing in-vitro drug release of 99.52% over a 12hrs extended period. FTIR studies revealed no interaction between drug and excipients used. The results of In-vivo kinetic studies are approving the better performance of the optimized formulation in comparison to marketed formulation, The Cmax, Tmax, half-life AUC values are confirming the same thing. In conclusion, Formulation (F11) was selected as optimized formulations could be offered as shows optimum sustained drug release compared to commercial formulation. Hence Meloxicam containing Chitosan as drug release controll


Author(s):  
Ritesh Kumar ◽  
Kashmira J. Gohil

Objective: The aim of the present study was to increase the absolute bioavailability of famotidine, enhanced patient compliance in the treatment of peptic ulcer by increasing its gastric residence time and controlled local release of drug upto 12 hours. Materials and Methods: Hydrodynamically balanced capsules of famotidine were prepared, consisting of floating matrix granules, which formed hydrogels. Effects of different formulation variables namely hypromellose (HPMC 4000 cps, HPMC 5600 cps, HPMC 15000 cps), effervescent agent (potassium bicarbonate) and mixing time were studied. Optimization study included 23 full factorial design with t50% and t80% as the kinetic parameters (response variable). Matrix characterization included scanning electron microscopy. All prepared formulations were evaluated to various parameters such as micromeritics properties, % buoyancy and in vitro drug release studies. Results and Discussion: The optimized formulation (F4) remains buoyant for more than 12 hrs. The in-vitro drug release study indicated that increasing the viscosity of HPMC resulted in sustained drug release with long floating duration. SEM studies showed definite entrapment of the drug in the matrix and hydrogel formation. Results showed a pH independent but polymer viscosity dependent drug release profile. The release kinetics followed Higuchi model and mechanism of release was found to be non-Fickian diffusion. Conclusion: Famotidine-loaded hydrodynamically balanced capsules were successfully prepared and prove to be useful for prolonged gastric residence of the drug, better bioavailability, patient compliance and improve delivery for enhanced anti-ulcer activity.


Author(s):  
ANKITA TIWARI ◽  
SANJAY K. JAIN

Objective: The present investigation aimed to develop and characterize Eudragit S-100 coated alginate beads bearing oxaliplatin loaded liposomes for colon-specific drug delivery. Methods: Liposomes were formulated by the thin-film hydration method. The process and formulation variables were optimized by Box-Behnken design (BBD) with the help of Design-Expert® Software. Three independent variables taken were HSPC: Chol molar ratio (X1), hydration time (X2), and sonication time (X3). The response variables selected were entrapment efficiency of oxaliplatin, polydispersity index, and vesicle size. Results: The liposomes possessed an average vesicle size of 110.1±2.8 nm, PDI 0.096±0.3, zeta potential of-6.70±1.4 mV, and entrapment efficiency of 27.65%. The beads were characterized for their size, in vitro drug release, and swelling index. The degree of swelling of the beads was found to be 2.3 fold higher at pH 7.4 than at pH 1.2. The in vitro drug release depicted a sustained drug release in 48 h. Conclusion: The outcomes of the study proposed that the developed system can be effectively used for site-specific drug delivery to the colon via the oral route.


Author(s):  
SUCHISMITA MOHANTY ◽  
SUBRATA SARANGI ◽  
GOURI SANKAR ROY

Objective: The purpose of the present study was to functionalized graphene (f-GE) grafted chitosan (CS)/Polyaniline (PANI) with Montmorillonite (MMT) was different feed ratio known as f-GE-g-(CS/MMT-PANI). Methods: The prepared f-GE-g-(CS/MMT-PANI) was formulated using the solvent casting method. The prepared nanocomposites were characterized by X-Ray Diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), Scanning electron microscope (SEM), Thermogravimetric analysis (TGA), thermogravimetric (DTG) and swelling in stimulated in the different biological fluid. The model drug Doxorubicin (DOX) was used for controlled drug delivery purpose. Results: From FTIR result was clearly demonstrated that the model drug DOX did not change in any molecular level at f-GE-(CS/MMT-PANI) (i.e. at<10 nm scale). Additionally, in DSC result, DOX was interacted with nanocomposites at scale>100 nm level. With CS as the carrier, 60% of the drug was released in SIF for the initial 120 min and this increased to 80–82% with f-GE-g-CS/MMT/PANI matrix. But in SGF, CS as the carrier, 46% of the drug was released in 140 min and this increased to 78% with f-GE-g-CS/MMT/PANI. In vitro drug release system was carried out by Korsmeyer Peppas’s power law. DOX and other drugs like Doxorubicin (DOX) was presented an exceptional higher drug result in different pH medium. Conclusion: It was observed that CS/MMT was decreasing less drug release rate compared to f-GE-g-(CS/MMT-PANI). So that it can be clearly understood that f-GE-g-(CS/MMT-PANI) grafted nanocomposites have enhanced drug release activity in different pH medium.


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