PRONIOSOMAL POWDERED DRUG DELIVERY SYSTEM OF FLURBIPROFEN :FORMULATION AND EVALUATION
*Sunil kumar, Amit kumar shahi, Ravi shanker, R. singh, Dr. R. ParthSarthy, Dr S.K. Prajapati
Kamla Nehru institute of technology and management, Sultanpur.
Bundelkhand university, Department of pharmacy, Jhansi
The purpose of this research is to design proniosomal powder drug delivery system of flurbiprofen in a trial to overcome the adverse effects associated with oral administration of the drug. Conventional chemotherapy for the treatment of intracellular infection is no more effective due to limited permeation of drug into cell. This can be overcome by the use of vesicular drug delivery system. Encapsulation of a drug in vesicular structure can be predicted to prolong the existence of the drug in the systemic circulation and thus enhance penetration into target tissue and reduce toxicity.Proniosomal powder are generally present in transparent, translucent or white texture, which makes them physically stable during storage and transport. Due to the limited solvent system present, the proniosomes formed were the mixture of many phases of liquid crystal, viz. lamellar, hexagonal and cubic phase liquid crystals.The potential of proniosomes as a transdermal drug delivery system for flurbiprofenwas investigated by encapsulating the drug in various formulations of proniosomal powder composed of various ratios of sorbitan fatty acid esters, cholesterol, prepared by slurry method. The formulated systems were characterized in vitro for size, vesicle count, drug entrapment, drug release profiles and vesicular stability at different storage conditions. Stability studies for proniosomal powder were carried out for 4 weeks. The method of proniosome loading resulted in an encapsulation yield of 30.6 – 75.4%. Proniosomes were characterised by transmission electron microscopy. In vitro studies showed prolonged release of entrapped flurbiprofen. At refrigerated conditions, higher drug retention was observed. It is evident from this study that proniosomes are a promising prolonged delivery system for captopril and have reasonably good stability characteristics.
Reference ID: PHARMATUTOR-ART-1322
Non-ionic surfactant vesicles known as niosomes are microscopic lamellar structures formed on admixture of a non-ionic surfactant, cholesterol and dicetyl phosphate with subsequent hydration in aqueous media. Proniosomes offer a versatile vesicle drug delivery concept with potential for delivery of drugs via transdermal route. This would be possible if proniosomes form niosomes upon hydration with water from skin following topical application under occlusive conditions. Proniosomes minimizes problems of niosomes physical stability such as aggregation, fusion and leaking and provide additional convenience in transportation, storage and dosing. Transdermal therapeutic system has generated an interest as this system provides the considerable advantage of a non-invasive parenteral route for drug therapy, avoidance of first pass gut and hepatic metabolism, decreased side effects and relative ease of drug input termination in problematic cases.Provesicular systems had attracted researchers as an alternate strategy for transdermal delivery of drugs because of the non-toxicity and penetration effect of lecithin/surfactants. Provesicular systems have been exploited in oral drug delivery in the form of tablets, beads or capsules and have shown improved dissolution and absorption characteristics. Based on the investigations provesicular systems appear to be an alternate drug carrier for various routes of drug administration.Flurbiprofen, are nonsteroidal anti-inflammatory drug (NSAIDs) is used for the relief of pain and inflammation associated with rheumatoid arthritis and osteoarthritis. It exhibits anti-inflammatory, analgesic and antipyretic activities. It is also used in mild to moderated pain including dysmenorrheal and migraine. Flurbiprofen is more potent than Ibuprofen but has more gastric side effectlike peptic ulceration and severe gastrointestinal bleeding may occurs. This drug may also cause serious effect on stomach or intestine including bleeding or perforation (forming of hole). The plasma half life (t1/2) of flurbiprofen is 4-6 hours. Hence repeated administration of high dose (100 mg: three time a day) is required for effective management of rheumatoid arthritis and osteoarthritis.It will be also effected the transdermal system rate because of its size, nature and chemistry, these systems give better drug permeability from biological bioavailability membranes and helps in solubilization of some practically insoluble drugs and hence solve problems of many drug.
To overcome the problem like gastric side effect, short half life and low bioavailability etc of flurbiprofen can be solved by developing the formulation of flurbiprofen as proniosome carriers in the form powder.
Flurbiprofen was a gift from F.D.C. Mumbai, cholesterol, and dialysis tubing were purchased from Hi-Media Laboratories (Mumbai, India). Span 20, 40, 60, 80 and BRIJ 35 were purchased from Central Drug House (Delhi, India).All other chemicals and solvents were of annular grade and obtained from C.D.H Company for pharmaceutical chemicals,(Delhi, India).
Proniosomes were prepared by Slurry method.
Strategies for the preparation of provesicles in the preparation of proniosomes non-ionic surfactants, coating carriers and membrane stabilizers are commonly used. The non-ionic surfactants used are Span (20, 40, 60, 80, Brij 35). The coating carriers used is maltodextrin (Maltrin M500, M700), membrane stabilizers like cholesterol are also used.
For ease of preparation a stock solution of accurately weighted quantities of surfactant, cholesterol and drug was prepared in 10 ml chloroform: methanol (2:1) solution the required volume of surfactant, cholesterol stock solution and drug was added to a 100 ml round bottom flask containing 500 mg maltodextrin carriers. Additional chloroform: methanol solution was added to form slurry in the case of lower surfactant loading. The flask was attached to a rotary evaporator to evaporate solvent at 60-70 rpm, a temperature of 45±2ºc and a reduced pressure of 600 mmhg. Until the mass in the flask had become a dry free flowing product. These materials were further dried overnight in desecator under vaccum at room temperature. This dry preparation is referred to as Proniosomes Powder.
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