GROUP 5: DHRUANSH MEHTA 20BPH017 PRITI MOHITE 20BPH020 AARKEE PARIKH 20BPH027 FORAM PARMAR 20BPH029 JAYENDRA SHARMA 20BPH094 WHAT IS FLOATING MICROSPHERE SYSTEM? A floating microsphere system is a drug delivery technology that releases medication into the stomach or upper digestive tract in a controlled and long-lasting manner. The microspheres are usually made of biocompatible polymers floating on the stomach acid’s surface. This buoyancy helps to keep the drug-loaded microspheres in contact with the stomach lining which is useful for drugs that require targeted delivery or low solubility in a gastric environment. SELECT A SUITABLE DRUG CANDIDATE FOR THE FLOATING MICROSPHERE SYSTEM The suitable drug candidate that can be used for this delivery system is: “RANITIDINE” • Ranitidine is an H2 receptor antagonist commonly used to treat conditions related to excessive stomach acid production such as peptic ulcers and gastroesophageal reflux disease[GERD]. • Controlled release via floating microspheres can enhance its efficacy in reducing stomach acid production. TARGET DELIVERY: It refers to the specific and controlled transport of a drug to a particular site within the body, intending to optimize its therapeutic effect while minimizing side effects. • Stomach targeting: Floating microspheres are designed to float on the gastric fluid due to their lower density. The stomach is the primary target for conditions like peptic ulcers, acid reflux, and some infections. • Buoyancy mechanism: Floating microspheres are formulated to have a lower density than gastric fluid, allowing them to float on the stomach’s surface. RELEASE RATE: • The goal is to prolong the residence time of the microsphere in the stomach, allowing for controlled and sustained drug release. They are generally formulated to provide controlled drug release, maintaining the therapeutic levels. • The desired release rate depends on the specific drug and condition being treated. • Release rate may be in a range of 8 to 12 hours. • The release of ranitidine is intended to occur at a higher pH, which is more alkaline around pH 3.5 to 5.5. The pH-dependentchanges release can also be engineered into this system by selecting polymers and excipients that respond to change in pH. POLYMER SELECTION: Several different substances both biodegradable as well as nonbiodegradable have been investigated for the preparation of microspheres. The specific polymers used for the preparation of the ranitidine floating microsphere are: • Ethyl Cellulose: It is a hydrophobic polymer that can be used to create microspheres with controlled release properties and it is often employed to encapsulate drugs. They provide buoyancy that ensures the floating of microspheres on the surface. • Polyethylene Glycol [PEG]: It is used in solubility enhancement as well as acts as a plasticizer to improve flexibility and mechanical properties. PEG can enhance the compatibility between the drug and the polymer used. • Eudragit: Eudragit RL and RS, are often used as they offer flexibility. • Chitosan: It is a biocompatible polymer that can enhance the gastric retention of microspheres, which is beneficial for ranitidine that requires prolonged action in the stomach. PATIENT COMPLIANCE: • Reducing dosing frequency: Microspheres are extended to provide an extended and controlled release of ranitidine. This allows for less frequent dosing, such as once a day which significantly improves patient compliance. • Ease Of Use: Floating microspheres are typically encapsulated in oral dosage forms. Ensure that the dosage form is not too large or difficult for the patients to swallow. • Taste Masking: Ranitidine has a bitter taste so taste masking techniques make the formulation more palatable for the patients, which encourages them to take medicaments on time. • Minimizing Side Effects: Select polymers and excipients that minimize the potential side effects, especially gastrointestinal discomfort or irritation. This can enhance patient comfort and willingness to continue the treatment. ADVANTAGES • Enhanced bioavailability • Enhanced first-pass biotransformation • Sustained drug delivery/reduced frequency of dosing • Flexibility in dosage form design. • A sustained mode of drug release enables the extension of the time over a critical concentration and thus enhances pharmacological effects and improves clinical outcomes. • Minimizes the counter activity of the body leading to higher drug efficiency. • Site-specific drug delivery. • Minimized adverse activity in the colon • Reduced fluctuations in drug concentration REFERNCES: • https://www.researchgate.net/publication/261513544_Floating_Microspheres_as_Drug_Delivery_S ystem • Jain SK, Agrawal GP, Jain NK. Floating microspheres as drug delivery system: newer approaches. Curr Drug Deliv. 2008 Jul;5(3):220-3. doi: 10.2174/156720108784911721. PMID: 18673266. • https://doi.org/10.1016/j.ijpharm.2008.02.02 4
