scholarly journals Synthesis Characterization of Platinum (IV) Complex Curcumin Backboned Polyprodrugs: In Vitro Drug Release Anticancer Activity

Polymers ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 67
Author(s):  
Honglei Zhang ◽  
Yanjuan Wu ◽  
Xiao Xu ◽  
Chen Chen ◽  
Xiukun Xue ◽  
...  
Keyword(s):  
Drug Release ◽  
Combination Chemotherapy ◽  
In Situ Polymerization ◽  
Average Diameter ◽  
Monomethyl Ether ◽  
Resistant Cell ◽  
Burst Release ◽  
Tumor Resistance ◽  
In Vitro Drug Release

The conventional mono-chemotherapy still suffers from unsatisfied potency for cancer therapy due to tumor heterogeneity and the occurrence of drug resistance. Combination chemotherapy based on the nanosized drug delivery systems (nDDSs) has been developed as a promising platform to circumvent the limitations of mono-chemotherapy. In this work, starting from cisplatin and curcumin (Cur), we prepared a dual drug backboned shattering polymeric nDDS for synergistic chemotherapy. By in situ polymerization of the Cur, platinum (IV) complex-based prodrug monomer (DHP), L-lysine diisocyanate (LDI), and then conjugation with a hydrophilic poly (ethylene glycol) monomethyl ether (mPEG) derivative, a backbone-type platinum (IV) and Cur linkage containing mPEG-poly(platinum-co-Cur)-mPEG (PCPt) copolymer was synthesized. Notably, the platinum (IV) (Pt (IV)) and Cur were incorporated into the hydrophobic segment of PCPt with the fixed drugs loading ratio and high drugs loading content. The batch-to-batch variability could be decreased. The resulting prodrug copolymer then self-assembled into nanoparticles (PCPt NPs) with an average diameter around 100 nm, to formulate a synergetic nDDS. Importantly, PCPt NPs could greatly improve the solubility and stability of Cur. In vitro drug release profiles have demonstrated that PCPt NPs were stable in PBS 7.4, rapid burst release was greatly decreased, and the Pt and Cur release could be largely enhanced under reductive conditions due to the complete dissociation of the hydrophobic main chain of PCPt. In vitro cell viability test indicated that PCPt NPs were efficient synergistic chemotherapy units. Moreover, PCPt NPs were synergistic for cisplatin-resistant cell lines A549/DDP cells, and they exhibited excellent reversal ability of tumor resistance to cisplatin. This work provides a promising strategy for the design and synthesis of nDDS for combination chemotherapy.

scholarly journals DESIGN AND DEVELOPMENT OF TOPICAL HYDROGEL FORMULATION OF IRBISARTAN

2019 ◽  
pp. 79-83
Author(s):  
ZEESHAN SHAIKH
Keyword(s):  
Angiotensin Ii ◽  
Drug Release ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Burst Release ◽  
Angiotensin Ii Receptor ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir

Objective: Irbesartan is an antihypertensive with limited bioavailability. The objective of the study was to develop controlled release matrix tablets of irbisartan drug. Methods: Tablets were prepared by wet granulation process. Result: In vitro drug release study revealed that HPMC causes initial burst release of drug hence combining HPMC sustained the action for 8 h (95.92±0.57% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism for drug release. Compared to conventional tablets, the release of model drug from these HPMC matrix tablets was prolonged, leading to achieve an effective therapy with a low dosage of the drug, to reduce the frequency of medication. The pharmacological and clinical properties of irbesartan, a noncompetitive angiotensin II receptor type 1 antagonist, successfully used for more than a decade in the treatment of essential hypertension. Results: Compatibility Studies In order to investigate the possible interactions between irbesartan and distinct polymers and/or diluents, FT-IR and DSC studies were carried out. FT-IR results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug and also drug excipients mixture. In picture 1 and 2. DSC studies indicate that chosen excipients for the formulation were found to be compatible with the active ingredient as the melting endothermic peaks are in the range of 250-320 °C which is same as the melting point of irbisartan. Conclusion: Irbesartan exerts its antihypertensive effect through an inhibitory effect on the pressure response to angiotensin II. Irbesartan 150–300 mg once daily confers a lasting effect over 24 h, and its antihypertensive efficacy is further enhanced by the coadministration of hydrochlorothiazide.

Development and Evaluation of Guaifenesin Bilayer Tablet

2010 ◽  
Vol 3 (3) ◽  
pp. 1122-1128 ◽  
Author(s):  
Vijaya Kumar B ◽  
Prasad G ◽  
Ganesh B ◽  
Swathi C ◽  
Rashmi A ◽  
...  
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Drug Content ◽  
Bilayer Tablet

The objective of the present research was to develop a Bilayer tablet of guaifenesin (GBT) using superdisintegrant MCC and sodium starch glycolate for the fast release layer and metalose 90 SH and carbopol 934 for the sustaining layer. The guaifenesin SR granules of different formulation were evaluated for bulk density, tapped density, angle of repose, Carr’s index and Hausners ratio and results were found to be 0.460 ± 0.12 to 0.515 ± 0.03 gm/cm3 , 0.550 ±0.03 to 0.590 ±0.04 gm/cm3 , 19 ±0.01 to 26 ± 0.23, 13.72 ± 0.03 to 19.56 ± 0.04 & 1.137 to 1.196, respectively. The prepared bilayer tablets were evaluated for weight variation, hardness, friability, drug content and in vitro drug release. In vitro dissolution studies were carried out in a USP 24 apparatus I. The formulations gave an initial burst effect to provide the loading dose of the drug followed by sustained release for 12 h from the sustaining layer of matrix embedded tablets. In vitro dissolution kinetics followed the Higuchi model via a non-Fickian diffusion controlled release mechanism after the initial burst release. Stability studies conducted for optimized formulation did not show any change in physical appearance, drug content, matrix integrity and in vitro drug release. The results of the present study clearly indicated that GBT was a stable dosage form and a promising potential of the guaifenesin bilayer system as an alternative to the conventional dosage forms

scholarly journals PREPARATION AND CHARACTERIZATION OF CEFTRIAXONE SODIUM ENCAPSULATED CHITOSAN NANOPARTICLES

2017 ◽  
Vol 9 (6) ◽  
pp. 10 ◽  
Author(s):  
P. Manimekalai ◽  
R. Dhanalakshmi ◽  
R. Manavalan
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Chitosan Nanoparticles ◽  
Cross Linking ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Cumulative Percentage ◽  
Ceftriaxone Sodium

Objective: The objective of this study was to prepare ceftriaxone sodium chitosan nanoparticles (CS-NP) from different drug and polymer ratios and analyze their physicochemical characteristics.Methods: Ceftriaxone sodium loaded chitosan nanoparticles were prepared using chitosan as a polymer and tri sodium polyphosphate (TPP) as cross linking agent by ionic cross linking and coacervation with the aid of sonication. Various trials have been carried out for the confirmation of nanoformulation. Parameters such as the zeta potential, polydispersity, particle size, entrapment efficiency, in vitro drug release Thermo gravimetric analysis and scanning electron microscope of the nanoparticles were assessed for confirmation of nanoformulation.Results: The formulated nanoparticles showed mean particle size, polydispersity index and zeta potential to be 183.1±8.42 nm, 0.212±0.05, +38.5±1.6 mV respectively and the drug loading was found to be 46.42±10 %. In vitro drug release was showed a biphasic release pattern with initial burst release followed by sustained release of formulated nanoparticles. The cumulative percentage of drug release was about 83.08 %.Conclusion: Formulation F2 was found to be the best formulation with a higher cumulative percentage of drug release. Modified ionic gelation method can be utilized for the development of chitosan nanoparticles of ceftriaxone sodium. Polymer and crosslinking agent concentrations and sonication time are rate-limiting factors for the development of the optimized formulation. The chitosan nanoparticles developed would be capable of sustained delivery of ceftriaxone sodium.

In vitro drug release and antibacterial activity evaluation of silk fibroin coated vancomycin hydrochloride loaded poly (lactic-co-glycolic acid) (PLGA) sustained release microspheres

2022 ◽  
pp. 088532822110640
Author(s):  
Shengtang Li ◽  
Xuewen Shi ◽  
Bo Xu ◽  
Jian Wang ◽  
Peng Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Burst Release ◽  
Plga Microspheres ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Initial Burst Release

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

Biodegradable Amphiphilic Tri-Block Copolymeric Nanoparticles for Controlled MTB Drug Delivery

2012 ◽  
Vol 584 ◽  
pp. 460-464 ◽  
Author(s):  
M Gajendiran ◽  
S. Balasubramanian
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Powder Xrd ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Loading Efficiency ◽  
Release Studies ◽  
Drug Loading Efficiency

. A series of biodegradable amphiphilic tri-block copolymers (PLGA–PEG–PLGA) have been derived from the diblock copolymer poly (lactic–co–glycolic acid (PLGA)) and polyethylene glycol (PEG). The mycobacterium tuberculosis (MTB) drug pyrazinamide (PZA) loaded polymer nanoparticles (NPs) have been prepared by probe-sonication followed by w/o/w double emulsification technique. The copolymers have been characterized by FTIR and 1HNMR spectroscopic techniques, TG-DTA analysis, GPC analysis and powder XRD pattern. The MTB drug loaded polymeric NPs have been characterized by FESEM, powder XRD, HRTEM and XPS analysis. The drug loading efficiency, drug content and in vitro drug release studies have been carried out by spectrophotometry. The drug loading efficiency and drug content of triblock copolymeric NPs were higher than these of diblock copolymeric microparticles (MPs). The in vitro drug release studies indicate that the NPs exhibit initial burst release followed by controlled release of PZA for longer durations. The drug release kinetics mechanism has been evaluated by zero order, first order, Korsemeyer-Peppas (KP) and Higuchi models.

scholarly journals Frovatriptan Succinate Loaded Lipid Nanoparticles: Formulation, Evaluation, Stability Study and Shelf Life Determination

2021 ◽  
pp. 266-274
Author(s):  
Mohd Yasir ◽  
Iti Chauhan ◽  
Madhu Verma ◽  
KM Noorulla ◽  
Abdurazak J. Tura ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Shelf Life ◽  
Lipid Nanoparticles ◽  
Stability Study ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Release Pattern

Aims: The aim of the research work was to prepare and optimize the Frovatriptan Succinate (FVN) loaded solid lipid nanoparticles. Methods: SLNs were developed by solvent  emulsification diffusion technique and evaluated for particle size, PDI, zeta potential, in-vitro drug release, and finally stability study was conducted for the detection of shelf life. Results: The optimized formulation exhibited particle size, PDI, and zeta potential 122.85±9.24 nm, 0.129 and -25.85 mV, respectively.  In-vitro drug release study exhibited  biphasic drug release pattern.  Initially (in first two hrs) the drug was release in fast manor i.e. burst release (32.36±7.28 %). It might be due to the presence of drug on the surface of SLNs. After  2 hrs of study, the release pattern became sustained up to 24 hrs. The total amount of drug release in 24 h was found to be 91.29 ± 8.26%.  Various kinetic models were applied to evaluate the release pattern of the drug form the formulation.  Higuchi model was found to be the best fitted with the R2 value of 0.9482. The release mechanism was found to be the Fickian type with the release exponent (n) value of 0.4386. Finally, stability study was conducted. The formulation was found to be the stable under the studied conditions. The shelf life of the formulation was found to be 1.77 years. Conclusion: Finally, it could be concluded that, the SLNs are the suitable carrier for the delivery of FVN .

scholarly journals DEVELOPMENT AND EVALUATION OF NANOSPONGES LOADED EXTENDED RELEASE TABLETS OF LANSOPRAZOLE

2019 ◽  
Author(s):  
Dingwoke John Emeka Francis ◽  
Felix Sunday Yusuf
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Average Diameter ◽  
Powder Flow ◽  
Solvent Evaporation Method ◽  
Flow Properties ◽  
In Vitro Drug Release ◽  
Drug Molecules ◽  
Optimum Formulation

Nanosponges are tiny sponges with an average diameter below 1µm and consist of cavities filled with drug molecules. Lansoprazole is one of the classes of proton pump inhibitors, it reduces gastric acidity, and used in disorders such as gastric ulcer, duodenal ulcer and reflux oesophagitis.   In present study for extended delivery of lansoprazole at optimal concentration and to reduce the frequency of dosing and thus to increase patient convenience nanosponges loaded extended release tablets were prepared. Initially four different nanosponges formulations were prepared by solvent evaporation method and evaluated on various parameters. Ethyl cellulose was used as entrapping agent and dichloromethane as cross linking agent in various proportions and evaluated for powder flow properties, % yield, zeta potential, and in-vitro drug release characteristics. Based on the evaluation results, formulation NS1 was selected to prepare five extended release tablets formulations by using HPMC K30 and chitosan as extended release polymers. All five formulations were evaluated for thickness, hardness, friability, % drug content and in-vitro drug release. From the results, it was found that all the evaluation results are within pharmacopoeial limits. From this study, we concluded feasibility of extended release of Lansoprazole through nanosponge loaded extended release tablets. Formulation of batch NT1, containing HPMC K30 was found to be optimum formulation.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

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.

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

2018 ◽  
Vol 8 (2) ◽  
Author(s):  
Dillip Kumar Behera ◽  
Kampal Mishra ◽  
Padmolochan Nayak
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Nanocomposite Films ◽  
Casting Method ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Clay Particles ◽  
Solution Casting Method ◽  
Nanoclay Content

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.

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