scholarly journals Facile Fabrication of Composite Scaffolds for Long-Term Controlled Dual Drug Release

2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Dawei Li ◽  
Chao Li ◽  
Xing Wang ◽  
Chunlin Li ◽  
Tunan Sun ◽  
...  

Bone tuberculosis (TB) caused by mycobacterium tuberculosis continues to present a formidable challenge to humans. To effectively cure serious bone TB, a novel kind of composite scaffolds with long-term dual drug release behaviours were prepared to satisfy the needs of both bone regeneration and antituberculosis drug therapy. In virtue of an improved O/W emulsion technique, water-soluble isoniazid (INH)-loaded gelatin microparticles were obtained by tailoring the content of β-tricalcium phosphate (β-TCP), which played significant roles in INH entrapment efficiency and drug release behaviours. By mixing with the poly(ε-caprolactone)-block-poly (lactic-co-glycolic acid) (b-PLGC) solution containing oil-soluble rifampicin (RFP) via the particle leaching combined with phase separation technique, the dual drugs-loaded composite scaffolds were fabricated, which possessed interconnected porous structures and achieved the steady release of INH and RFP drugs for three months. Moreover, this dual drugs-loaded system could basically achieve their expectant roles of respective drugs without obvious influences with each other. This strategy on preparation of intelligent composite scaffolds with the multi-drugs loading capacity and controlled long-term release behaviour will be potential and promising substrates in clinical treatment of bone tuberculosis.

2015 ◽  
Vol 486 (1-2) ◽  
pp. 30-37 ◽  
Author(s):  
J.L. Paris ◽  
J. Román ◽  
M. Manzano ◽  
M.V. Cabañas ◽  
M. Vallet-Regí

Author(s):  
Deevan Paul A. ◽  
Avilala Neelima ◽  
Chitra Prasanthi ◽  
Navyaja Kota

Clopidogrel bisulphate (CB) is a crystalline, poorly water-soluble drug of bioavailability less than 50%. The drug is an irreversible inhibitor of the P2Y12 adenosine diphosphate receptor found on the membranes of platelet cells. The present work was performed using different polymers such as Polyvinylpyrrolidone (PVP) K-30 and polyvinyl alcohol with varied surfactants such as Tween 80 in comparison by using superdisintegrants like Sodium Starch Glycolate (SSG) and Microcrystalline Cellulose (MCC). By performing the particle size distribution, the size ranges from 232.6 nm to 995.6 nm and the polydispersity index ranges from 0.11 to 0.96, these ranges indicating the good physical nature of nanoparticles. The drug entrapment efficiency (DEE) of clopidogrel bisulphate nanoparticles was found to be in the range of 30.10% to 94.4%. From the study, it was found that F2 formulation containing PVP K-30 and L-arginine has given the best release in 80mins and the maximum cumulative drug release was 96.8% in comparison with other formulation, and the dissolution studies were performed for the seven formulations of prepared clopidogrel bisulphate granules among which F5 formulation containing crospovidone has given maximum drug release of 91.6% within 80mins. Here we state that the method development technologies improve the solubility and bioavailability studies by producing the nanoparticles.


2021 ◽  
Vol 11 (5) ◽  
pp. 110-114
Author(s):  
Harshita Jain ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar

The guanine derivative antiviral drug acyclovir (ACV) is one of the oldest molecules put downing triumphant market until date, being commercially accessible in a variety of dosage forms for oral, topical and parenteral administrations. Clinical purpose of this drug is better to new antiviral agents due to its potential values such as suppression of recurrence, security profile, negligible drug interactions and being inexpensive. ACV is slightly water soluble, less permeable and poorly bioavailable, yet further potential antiviral molecule, the physicochemical alterations and new dosage form approaches resulted with more than 100 research efforts within a decade. The current study endeavored at the formulation of chitosan microspheres loaded with ACV to conquer the poor bioavailability and recurrent dose administration. Chitosan microspheres were prepared by emulsification technique by glutaraldehyde cross-linking. A variety of formulation and process variables such as polymer, glutaraldehyde, drug, span 80 concentrations, effect of stirring speed and stirring time were optimized. Formulated microspheres were characterized for its drug loading, invitro drug release, entrapment efficiency, surface morphology (SEM), particle size analysis and FTIR spectroscopy. The characterization of the fabricated microspheres demonstrated smooth surface with thin particle size allocation and entrapment efficiency of 80.8% for stirring speed batch. The prepared microspheres showed a controlled drug release of 93.2% over a period of 8 hrs with initial burst release of 56.7 % in the first 2hrs. The FTIR showed that there was no possible drug interaction among the drug and polymer. From the data’s obtained it can be concluded that the chitosan microspheres could be believed as a possible carrier for controlled drug delivery of ACV. Keywords: Acyclovir, Antiviral drug, Microspheres, Chitosan, Glutaraldehyde.


Author(s):  
SHAILESH SHARMA ◽  
NIMRATA SETH

Objective: In the present protocol, employability of polymethacrylate polymer Eudragit RS100 for development of microparticles of water soluble drug with desired values of response variables was investigated by central composite optimization design through application of Design Expert® software (Series DX10). Methods: The microparticles were developed by emulsion solvent evaporation process employing Eudragit RS100. Two effective independent variables drug: polymer ratio and stirring speed were selected to assess performance prospective of Eudragit on mean particle size, entrapment efficiency, percent yield and drug release in 12 h of microparticles. Thirteen batches generated by software were prepared and subjected to different characterization test parameters obligatory for the evaluation of formulation. Validation of optimization model and Statistical interpretation of results was done using Analysis of Variance (ANOVA) Results: ANOVA indicated that the independent variables had significant effect on response variables. Optimized formulation demonstrated close agreement amongst experimental and predicted responses with high desirability factor. In vitro drug liberation study for optimized formulation proposed a sustained release of drug from microparticles. Conclusion: In conclusion, optimization technique was imperative in indicating the efficient applicability of Eudragit RS100 polymer in controlling the drug release of hydrophilic drugs.


2019 ◽  
Vol 7 (7) ◽  
pp. 2975-2985 ◽  
Author(s):  
Han Cao ◽  
Yu Duan ◽  
Qinrui Lin ◽  
Yuhong Yang ◽  
Zuguang Gong ◽  
...  

A thixotropic injectable regenerated silk fibroin/hydroxypropylcellulose (RSF/HPC) hydrogel for highly sustainable dual-drug release with improved anticancer therapy and alleviated side effects.


Author(s):  
Ranjitha R ◽  
Elango K ◽  
Devi Damayanthi R ◽  
Sahul Hameed Niyaz U

The present investigations was aimed to improve the solubility, to release the drug in a controlled manner for extended period of time, reduce dose dependent side effects and improve the bioavailability of a poorly water soluble BCS class II drug of Lovastatin by formulating it as Nanosponges drug delivery system. Lovastatin Nanosponges were formulated by emulsion solvent evaporation method using Eudragit RS 100 and Ethyl Cellulose as a polymers, PVA as a stabilizer and finally enclosed in hard gelatin Capsules. The prepared Nanosponges were evaluated for FTIR, particle size, polydispersity index (PDI), zeta potential, morphological characteristics by scanning electron microscopy (SEM), production yield, entrapment efficiency, solubility studies, in vitro drug release studies, release kinetics study, stability studies, Flow property and porosity. The optimized formulation filled in capsules and Post formulation parameters of capsule were determined. FTIR studies showed no interaction between drug and excipients. Percentage yield of all the formulation (F1-F10) was found to be in the range of 85.83 to 99.85%. The entrapment efficiency of all the formulations was found to be in the range of 61.68 to 91.18%, among all the formulations F3 (90.04%) and F8 (91.18%) shows high entrapment efficiency. The solubility of all formulation improved (from insoluble to slightly soluble) compared to pure drug of Lovastatin. Among all the formulations F3 (98.15%) and F8 (97.57%) shown complete drug release at the end of 12th hrs. The average particle size of optimized formulation F3 and F8 was found to be 727.0 nm and 769.5 nm respectively. SEM images of optimized formulation showed that the Nanosponges were spherical with numerous pores on their surface, uniform and spongy in nature. The release kinetics of the optimized formulation was best fitted into Higuchi model and showed zero order drug release with Non Fickian diffusion. Stability studies indicated that the formulation is stable as per ICH guidelines. The flow property measurements for optimized formulation observed good were its filled in capsules. Post formulation parameters of capsule were comply with official specifications. They concluded that the both polymers used were efficient carriers for Lovastatin Nanosponges.


Author(s):  
Mousumi Kar ◽  
Houdhury Pratim ◽  
Sujit Pillai ◽  
Singh Nagendra

Alginate microspheres for a highly water soluble antidiabetic drug Metformin hydrochloride was prepared by ionic gelation method and investigated for its various physicochemical and release properties. To prevent a rapid drug release from alginate microspheres in simulated gastro-intestinal media, alginate microspheres were blended with polymers, hydroxy propyl methylcellulose, methylcellulose, chitin and chitosan and evaluated as additive polymers for controlling the drug release. Results indicated that quantity of polymer; gelating agent and time of cross-linking affected the shape, size and release characteristics from the prepared dosage forms. Use of polymers to retard the release of drug was effective. Drug release from the microspheres followed swelling and erosion. The selected batches sustained the release of the drug for more than 8 h. and showed drug entrapment efficiency up to 85%. As the polymer concentration in the formulation increased, the drug release generally decreased. HPMC-blended microspheres swelled but withstood the disintegration, showing an ideal linear release profiles. The zero order release was shown by all the formulations except when chitosan was incorporated. In comparison with chitosan-blended microspheres, HPMC-blended and MC blended alginate microspheres can be easily made and used for controlled drug delivery systems due to convenient process and better controlled drug release.


2015 ◽  
Vol 3 (17) ◽  
pp. 3436-3446 ◽  
Author(s):  
Ziming Yuan ◽  
Xin Zhao ◽  
Jingwen Zhao ◽  
Guoqing Pan ◽  
Wangwang Qiu ◽  
...  

A novel pH-sensitive electrospun composite PLLA fibrous scaffold was developed with long-term anti-cancer drug release and short-term anti-inflammation drug release for liver cancer therapy.


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