scholarly journals Preparation and Characterization of Intramuscular PLGA Based Microsphere

2019 ◽  
Vol 9 (5) ◽  
pp. 127-130
Author(s):  
Prateek Pathak ◽  
Sarvesh Paliwal

The current studies was design and evaluate biodegradable PLGA microspheres for sustained or extended release, with primary goal of avoiding combination of oral therapy for the treatment of schizophrenia. PLGA copolymers 75:25 was used to prepare four microsphere formulations of anti-psychotic drug Olanzapine. The microspheres were characterized by in-vitro dissolution and other physio-chemical methods. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state may be achieved by the second dose. Overall, the in-vitro study of Formulations 001, 002, 003, or 004 will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon duration of therapy. Results of this study prove the suitability of using PLGA 75:25 copolymers of different composition and molecular weight to produce sustained or extended release formulations that can enhance pharmacological effectiveness for anti-psychotic intra-muscular administration of Olanzapine. Keywords: sustained release, PLGA microspheres, Olanzapine

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Susan D’Souza ◽  
Jabar A. Faraj ◽  
Stefano Giovagnoli ◽  
Patrick P. DeLuca

The aim of this study was to design and evaluate biodegradable PLGA microspheres for sustained delivery of Risperidone, with an eventual goal of avoiding combination therapy for the treatment of schizophrenia. Two PLGA copolymers (50 : 50 and 75 : 25) were used to prepare four microsphere formulations of Risperidone. The microspheres were characterized by several in vitro techniques. In vivo studies in male Sprague-Dawley rats at 20 and 40 mg/kg doses revealed that all formulations exhibited an initial burst followed by sustained release of the active moiety. Additionally, formulations prepared with 50 : 50 PLGA had a shorter duration of action and lower cumulative AUC levels than the 75 : 25 PLGA microspheres. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state being achieved by the second dose. Overall, the clinical use of Formulations A, B, C, or D will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon cessation of therapy. Results of this study prove the suitability of using PLGA copolymers of varying composition and molecular weight to develop sustained release formulations that can tailor in vivo behavior and enhance pharmacological effectiveness of the drug.


Drug Delivery ◽  
2006 ◽  
Vol 13 (4) ◽  
pp. 277-285 ◽  
Author(s):  
Jaleh Varshosaz ◽  
N. Tavakoli ◽  
F. Roozbahani

2002 ◽  
Vol 234 (1-2) ◽  
pp. 195-203 ◽  
Author(s):  
Hak Soo Choi ◽  
Sun-Ah Seo ◽  
Gilson Khang ◽  
John M. Rhee ◽  
Hai Bang Lee

2011 ◽  
Vol 46 (10) ◽  
pp. 4878-4886 ◽  
Author(s):  
Azmat Ali Khan ◽  
Mahboob Alam ◽  
Saba Tufail ◽  
Jamal Mustafa ◽  
Mohammad Owais

Author(s):  
Naveen Goyal ◽  
Anil Kumar

Objective: The main objective of this research work was to design, prepare and evaluate extended release (ER) tablets of anti-asthmatic drugs (salbutamol sulphate and theophylline) by direct compression method using diverse ratios of hydroxypropyl methylcellulose (HPMC K100M) and ethyl cellulose (EC) along with some other excipients.Methods: Extended-release matrix tablets of salbutamol sulphate and theophylline were successfully fabricated by direct compression method and coded the formulations as F1 to F7 depending on the ratios of modified polymers. The core tablets composed of hydrophilic polymers of various ratios that allow the discharge of drugs at a controlled rate after coming in contact with the aqueous medium. The designed tablets were subjected to various assessment parameters i.e. friability test, hardness test, drug content consistency and In vitro dissolution tests.Results: Prepared formulations were subjected to various assessment parameters and the findings obtained were within the prescribed limit. To perform the in vitro drug dissolution tests of fabricated tablets, the calibration plots of pure drugs using various solvents i.e. 0.1N HCl, phosphate buffer (pH 6.8) and distilled water were plotted. Dosage forms F1-F7 containing ethyl cellulose and HPMC K100M in various concentration demonstrates the prolonged medications discharge for up to 8 h, among these formulations, F6 shows 95.32±0.24 % for salbutamol sulphate and 94.19±0.39 % for theophylline release at the end of 8 h. This finding reveals that a particular window of concentrations of ethylcellulose and HPMC K100M was capable of providing prolonged drugs discharge.Conclusion: The results obtained in this research work clearly showed a promising potential of extended-release tablets containing a specific ratio of HPMC K100M and ethylcellulose as a release rate controlling polymers for effective treatment of asthma and chronic obstructive pulmonary diseases (COPD).


1999 ◽  
Vol 18 (1) ◽  
pp. 12-16 ◽  
Author(s):  
E Tanaka ◽  
A Ishikawa ◽  
T Horie

Trimethadione (TMO) has the properties required of a probe drug for the evaluation of hepatic drug-oxidizing capacity and, in this study, we have summarized the in vivo and in vitro metabolism of TMO in various animal species including mouse, hamster, rat, rabbit, dog, monkey and human. In the in vivo study, the plasma TMO level was measured after intravenous or oral (human) administration of TMO at a dose of 4 mg/kg to various animal species. The rate of TMO metabolic clearance in these animal species in vivo was in the order mouse > hamster >rat>rabbit>dog>monkey>human. In the in vitro study, species differences were observed in the cytochrome P450 (P450) content and drug-oxidizing enzyme activity. The content of P450 was monkey> mouse>dog>rabbit>hamster>rat>human. On the other hand, TMO N-demethylation was in the order mouse >hamster >rat >rabbit>dog>monkey>human. There was a good correlation between the mean total body clearance of TMO ( in vivo)andthemeanTMON-demethylase activity ( in vitro) (y=1.7×+0.11, r=0.965, P<0.001). These results show that TMO is a probe agent with metabolic and pharmacokinetic characteristics making it attractive for the in vivo and in vitro characterization of metabolic activity in various animal species.


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