MICROENCAPSULATION

INTRODUCTION Microencapsulation is a process by which very tiny particles or droplets of solidor liquid material are coated or surrounded with a continuous film of polymeric material. These micro-capsules have a number of benefits such as converting liquids to solids, providing environmental protection, separating reactive compounds and improved material handling properties. Active materials are then encapsulated in micron-sized capsules of barrier polymers (gelatin, plastic, wax...). In the process of microencapsulation, tiny particles or droplets are surrounded by a coating to give small capsules with many useful properties. The material inside the microcapsule is referred to as Core, whereas the wall is called a shell, coating, or membrane [1]. An appropriate motto for studying micro encapsulation would be Small is better. Entrapment of a biologically active substance (from DNA to entire cell or group of cells) is known as Bioencapsulation, which is a part of microencapsulation [2]. Micro encapsulation involves the coatings of particles ranging dimensions from several tenths of a micron to 5000 micron in size and provides the means of converting liquids to solids, of altering surface and colloidal properties of providing environmental protection and of controlling the release characteristics or availability of coated materials [3]. The process targeted at creating a barrier between the core material in fine powder form or droplet form and its environment known as High performance micro encapsulation. Micro encapsulation is a process by which solids or liquids or even gases may be encapsulated into microscopic size particles through the formation of thin coating of wall material around the substance being encapsulated [4].

Reasons for Microencapsulation The main reason for microencapsulation is for sustained or prolonged release of the drug. This technique has been widely used for masking the organoleptic properties like taste and odor of many drugs and thus improves patient compliance e.g. Paracetamol, nitrofurantoine for masking the bitter taste. By using microencapsulation techniques the liquid drugs can be converted in a free flowing powder. The drugs can be protected by microencapsulation which is sensitive to moisture light and oxygen, such as nifedipine is protected from photo instability. Microencapsulation technique also helpful to prevent the incompability between drugs The drugs which are volatile in nature may vaporize at room temperature like Aspirin and peppermint oil can be prevented by microencapsulation. Reduction in toxicity and GI irritation including with KCL and ferrous sulphate can be achieved by microencapsulation Microencapsulation has also been employed to change the site of absorption. This application has been useful for those drugs which have the toxicity at lower pH. ADVANTAGES 1. Converts liquid into free flowing solid and pseudo solid which improves handling and storage like Eprazinone, Clofibrate, Castor oil, Cod-liver oil etc. 2. Reduces volatility of substances like methyl salicylate, peppermint oil, flavors, perfumes etc.

3. Avoid incompatibilities in drug combinations like aspirin and chlorpheniramine maleate, eutectic combinations etc. 4. Masks unpleasant taste of drug like penicillin derivatives like ampicillin, aminophylline, prednisolone, cod liver oil etc. 5. Mask unpleasant or unacceptable odor of cores like castor oil, cod liver oil, methionine, cysteine etc. 6. Reduces gastro intestinal irritation due to irritant drugs like ferrous sulphate, potassium chloride, paracetamol, phenylbutazone, indomethacin, nitrofurantoin etc. 7. Reduce hygroscopicity of core like sodium chloride etc. 8. Provides sustain / prolong / delay / control drug release. 9. Reduces hazards to operators in case of toxic chemicals like insecticides, pesticides and sensitizers like penicillins etc. 10. Improve flow properties, compaction and compressibility of the core like Vitamins etc. 11. For immobilization of enzymes for improving their stability and retention of activity. 12. By this chemical incompatible ingredients can produce in single form like Aspirin, Citric acid etc. 13. ADR are minimized DISADVANTAGE [3,7] Dose Dumping 1. Quite expensive, 2. The technique is not adaptable to all core materials, 3. Sometimes coating may be uncompleted and discontinuous, 4. No single method can be applied to all core materials, 5. Because of the inadequate stability and shelf life, Sensitive pharmaceuticals cannot used,

6. For different cores and different applications, Individual design approach is required, 7. Coated products may have non reproducible and unstable release characters, may be too bulky, 8. Limited choice of safe, approved, biocompatible and biodegradable materials, 9. May damage the coat or the product due to mechanical stress like compression, compaction, packaging, transport, handling etc. 10. Micro particles may not be suitable for parenteral applications due to size restrictions, 11. Need of sterilization, necessity of non-allergic, biocompatible and biodegradable nature of the carrier etc. 12. (Most information on microencapsulation is still patented and hence there may be difficulty in choosing suitable technique and methodology for individual applications, 13. There may be difficulties in scale up and large scale manufacturing the process.

APPLICATION OF MICROENCAPSULATION Microencapsulation technologies are applied in any area of the industry. It can be found in: (1) Cell immobilization In plant cell cultures microencapsulation, provides cell natural environment, improves efficiency in production of different metabolites used for medical, pharmacological and cosmetic purposes. Human tissue by microencapsulation are turned into bio-artificial organs in natural polymers and transplanted to control hormone-deficient diseases such as diabetes and severe cases of hepatic failure. In continuous fermentation processes immobilization is used to increase cell density, productivity and to avoid washout of the biological catalysts from the reactor and applied in ethanol and solvent production, sugar conversion or waste water treatment. (2) Beverage production Using immobilization technologies beverage products are beer, wine, vinegar and other food drinks production are to boost yield, improve quality, change aromas, etc... (3) Protection of molecules from other compounds Some chemicals are very dangerous for our body. Micro encapsulation solve simple problem like the difficulty to handle chemicals (detergents dangerous if directly exposed to human skin) as well as many other molecule inactive or incompatible if mixed in any formulation. (4) Drug delivery Microencapsulation has permitted controlled release delivery systems (allow controlling the rate, duration and distribution of the active drug.) after designing the right biodegradable polymers. One of the main advantages of such systems is to protect sensitive drug from drastic environment (pH,) and to reduce the number of drug administrations for patient and with these systems, micro

particles sensitive to the biological environment are designed to deliver an active drug in a sitespecific way (stomach, colon, heart and specific organs). (5) Quality and safety in food, agricultural & environmental sectors Encapsulated bio-systems enhanced development of the biosensors has been by used to control environmental pollution, food cold chain etc. (6) Soil inoculation Rhizobium bacteria which improves nitrate adsorption and conversion. But cells are washed out by rain so inoculation is often unsuccessful. By cell encapsulation processes, it is possible to maintain continuous inoculation and higher cell concentration. Nutraceuticals (e.g. probiotics, vitamins...)

improvement of their efficiency and stability by protecting and offering targeting release of the active materials (7)Pharmaceuticals In Pharmaceutical fields micro encapsulation is used to increase duration of action of drug, increase the stability of drug, increase the bioavailability, taste masking, increase the dissolving properties etc.

Evaluation
Morphology. Shape and surface morphology of microcapsules were studied using Scanning Electron Microscope (SEM, JSM 6100, Jeol, Japan). Particle sizes of the microcapsules were evaluated using optical microscope. Percentage Drug Content % Drug content= (Actual drug content of microcapsule/Theoritocal wt of drug in microcapsule)x100 Percentage encapsulation efficiency. %encapsulation efficiency = (%drug content/ %Theoretical drug content) X 100

Percentage yield % yield= (wt of microcapsules/Theroritical wt of drug and polymer )x100 Determination of swelling behavior. The water-sorption capacity of the microcapsules were determined by swelling 200 mg of dry microcapsules in phosphate-buffered saline (PBS) pH 7.4 for at least 24 hrs. The wet weight of the swollen microcapsules was determined by first blotting the microcapsules with filter paper to remove surface water and then weighed immediately. The percentage swelling of the microcapsules were calculated as: S = (We - Wo) / Wo x 100 % where, We denotes the weight of the gel microcapsules at equilibrium swelling and Wo the initial weight of the microcapsules.

In vitro wash-off test. The mucoadhesive property of the microcapsules was evaluated by the in-vitro wash-off test15,16 or in vitro adhesion testing method. The mucoadhesiveness of these microcapsules was compared with nonbioadhesive material, ethylene vinyl acetate microcapsules. Pieces of intestinal mucosa (2x2 cm.) were mounted on to glass slides (3x1 inch.) with cyanoacrylate glue. Two glass slides were connected with a suitable support. About 50 microcapsules were spread on to each wet rinsed tissue specimen and immediately thereafter the support was hung on to the arm of a U. S.P. tablet disintegrating test machine. A slow regular up and down moment was given in a test fluid at 37C in 1 L vessel of the machine. At the end of 30 min, 1 h and later at hourly intervals upto 12 hrs, the machine was stopped and the number of microcapsules still adhering on to the tissue was counted. The test was performed in 0.1 N HCl and in phosphate buffer of pH 7.4.

In vitro drug release. The in vitro drug release17 profiles from various formulations of microspheres ( about 500 mg) were studied in 900 ml of buffer with gastrointestinal simulated pH conditions, viz. simulated gastric fluid (0.1N HCl, pH 1.2) for first 2 hours followed by next 4 hours in simulated intestinal fluid (phosphate buffer solution, PBS, pH 6.8) and finally up to 15 h in simulated intestinal fluid (phosphate buffer solution, PBS, pH 7.4) at 100 rpm. At different time intervals, 10 ml. of samples were withdrawn and filtered through a 0.8 m cellulose acetate membrane filter and estimated .