MICROBALLOONS DELIVERY SYSTEM: AN INNOVATIVE ACCEPTABLE APPROACH IN GASTRORETENTIVE DRUG DELIVERY
Yashodhara Choubey*, Mr. Govind Bhandari, Mr. Avnish Sharma, Mr. Mukesh Mehra
Mahakal Institute of Pharmaceutical Studies,
Ujjain (M.P.), India
Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The Microballoons delivery systems are useful in such application. Microballoonsare gastro-retentive drug delivery systems based on non-effervescent approach. Microballoonsare in strict sense, spherical empty particles without core and ideally having a size less than 200 micrometer. Microballoonsare low-density systems that have sufficient buoyancy to float over gastric contents and remain in stomach for prolonged period. The drug is released slowly at desired rate resulting in increased gastric retention with reduced fluctuations in plasma drug concentration. Microballoons improve patient compliance by decreasing dosing frequency; better therapeutic effect of short half-life drugs can be achieved. These are primarily controlled release drug delivery systems, which gets retained in the stomach for longer periods of time, thus helping in absorption of drug for the intended duration of time. Gastric retentive drug delivery devices can be useful for the spatial and temporal delivery of many drugsbecause of buoyancy.
REFERENCE ID: PHARMATUTOR-ART-1892
Oral administration is the most convenient and preferred means of any drug delivery to the systematic circulation. Oral controlled release drug delivery have recently been of increasing interest in pharmaceutical field to achieve improved therapeutic advantages, such as ease of dosing administration, patient compliance and flexibility in formulation. Drugs that are easily absorbed from gastrointestinal tract (GIT) and have short half-lives are eliminated quickly from the systemic circulation. Frequent dosing of these drugs is required to achieve suitable therapeutic activity. To avoid this limitation, the development of oral sustained-controlled release formulations is an attempt to release the drug slowly into the gastrointestinal tract (GIT) and maintain an effective drug concentration in the systemic circulation for a long time. Microballoons is an approach to prolong the gastric retaintion which have a bulk density lower than gastric fluids and thus remain buoyant in stomach for a prolonged period of time, without affecting the gastric emptying rate. This results in an increase in gastric retention time and a better control of fluctuations in plasma drug concentrations. These microballoons are characteristically free flowing powders consisting of proteins or synthetic polymers, ideally having a size less than 200 micrometer.
ADVANTAGES OF MICROBALLOONS
1. Improves patient compliance by decreasing dosing frequency.
2. Bioavailability enhances despite first pass effect because fluctuations in plasma drug concentration is avoided, a desirable plasma drug concentration is maintained by continuous drug release.
3. Gastric retention time is increased because of buoyancy.
4. Enhanced absorption of drugs which solubilise only in stomach
5. Drug releases in controlled manner for prolonged period.
6. Site-specific drug delivery to stomach can be achieved.
7. Superior to single unit floating dosage forms as such microspheres releases drug uniformly and there is no risk of dose dumping.
8. Avoidance of gastric irritation, because of sustained release effect.
9. Better therapeutic effect of short half-life drugs can be achieved.
MECHANISM OF FLOATING MICROBALLOONS
When microballoonscome in contact with gastric fluid the gel formers, polysaccharides, and polymers hydrate to form a colloidal gel barrier that controls the rate of fluid penetration into the device and consequent drug release. As the exterior surface of the dosage form dissolves, the gel layer is maintained by the hydration of the adjacent hydrocolloid layer. The air trapped by the swollen polymer lowers the density and confers buoyancy to the microspheres. However a minimal gastric content needed to allow proper achievement of buoyancy.
Fig. Mechanism of floating systems, GF= Gastric fluid
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