Current Issue : October-December Volume : 2014 Issue Number : 4 Articles : 12 Articles
The Parenteral administration route is the most effective and common form of delivery for active drug substances with poor bio-availability and the drugs with a narrow therapeutic index. Though parenteral administration of drug is often critical and associated with problems such as limited number of acceptable excipients, stringent requirements of aseptic production process, safety issues and patient non-compliance. Still this route maintains its value due to special advantages like quicker onset of action in case of emergency, target the drug quickly to desired site of action, prevention of first pass metabolism etc. The Atrigel system is a proprietary delivery system that can be used for both parenteral and site-specific drug delivery. It consists of biodegradable polymers dissolved in a biocompatible carrier. When the liquid polymer system is placed in the body using standard needles and syringes, it solidifies upon contact with aqueous body fluids to form a solid implant. The ease of manufacture of the Atrigel system and its relatively pain-free subcutaneous injection into the body provide significant advantages over both solid implants and microparticles. Atrigel technology was licensed to the Atrix Laboratories. Atrigel technology currently used in cancer therapy, periodontal treatment and delivery of protein and peptide drugs. By using this technology we can delivered anaesthetics, antibiotics, vaccines, antipsychotics, hormones and NSAIDS in future. This review article complies the information on the in-situ gel forming system i.e. Atrigel technology designed to provide a more stable, ready-to-use formulation to provide drug release in sustained manner....
Ellagic acid, a polyphenolic compound derived from many dietary foods possesses diverse pharmacologic effects including anti-inflammatory, antioxidant, anticancer and antihypertensive activities in several oxidation-linked chronic diseases. Animal studies have shown that ellagic acid is safe and effective in many ailments but exhibit poor oral bioavailability. Different factors contributing to low bioavailability include poor absorption, metabolism in GIT, rapid distribution and elimination. Although, poor absorption and low systemic bioavailability of ellagic acid limit its clinical utilization, some of the methods for its use can be approached to enhance the absorption and achieve a therapeutic level of ellagic acid. These approaches involve, first, the use of amorphous solid dispersions (ASD) for improvement of solubility of ellagic acid; second, utilization of in situ gelling systems of ellagic acid; third, ellagic acid incorporated peptide microtubes; fourth, the use of liposomal curcumin; fifth, the use of niosomes of curcumin; and sixth, cyclodextrin inclusion complex of ellagic acid. Improved absorption or dissolution, bioavailability and therapeutic efficacy of ellagic acid after application of abovementioned approaches against various human diseases, including cancer, cardiovascular diseases, diabetes and neurological diseases has been documented. This indicates that in the near future bioavailability enhancement of ellagic acid is expected to boost this promising natural product to the lead of therapeutic agents for treatment of human disease....
The purpose of the study was to develop an optimized thermoreversible controlled release gel of amide group anesthetic agent for delivery into nasal mucosal pocket containing bupivacaine hydrochloride as a model drug. The prepared formulations are biocompatible and display low viscosity at the moment of in-vivo application. Once applied, formulation undergoes a sol-gel transition, resulting in semisolid gel. Thermosensitive controlled release gel containing 5% w/v bupivacaine hydrochloride was formulated by cold method using different combination of pluronic F 127, F 87, F 108 and F 68. The gels were evaluated for drug content, gelation temperature, viscosity, in-vitro release and ex-vivo evaluation of safety and efficacy of optimized formulation. The gelation of system at body temperature is important evaluation parameter in optimization study. The formulations containing 20% w/v of pluronic F 127, F 87, F 108 and 20% w/v of pluronic F 68 showed gelation near to body temperature. The drug release from the formulations was diffusion controlled without swelling. Ex-vivo evaluation of optimized formulation was carried in horizontal ussing chamber. Optimized formulation Af4, Af10, Af16 showed promising finding in management of pain associated with scaling and root planning. Site specific delivery of anesthesia with longer duration of action was achieved with thermoreversible gel....
The sustained release matrix tablets of cefpodoxime proxetil were prepared by direct compression techniques. The effect of hydrophilic matrices on the behavior of cefpodoxime proxetil using different polymers and their combinations. The prepared tablets were evaluated for various physico-chemical parameters. In-vitro release profile was check for 24 hrs to evaluate the SR matrix tablet of cefpodoxime proxetil. The drug release from the optimized formulation was found to follow zero order kinetics. Thus the phenomenon of drug release showed that the release of optimized formulation is controlled by diffusion. Administration of cefpodoxime proxetil in a sustained release dosage would be more desirable for bacterial infections effects by maintaining the plasma concentrations of the drug well above the therapeutic concentration. From in-vitro dissolution profile, batch F3 was prepared with blend of compritol® 888 ATO and hydroxypropyl methylcellulose (K15M) combination where drug release was about 98.11%....
The aim of the present study was to develop stable nanoparticulate formulation for sustained release of drug. Chitosan nanoparticles were prepared by ionic gelation method using tripolyphosphate as cross linking agent. Different nanoparticulate formulations were prepared by using 32 factorial design in which varying the concentration of chitosan (0.1% to 0.3%) and varying the concentration of tripolyphosphate (0.02% to 0.03%) as two factors. The effect of these factors on the particle size, % entrapment efficiency and in vitro drug release was evaluated to develop an optimized formulation. Particle size, % entrapment efficiency and in vitro release of optimized formulation was found to be 168.1nm, 78.53% and 70.80% respectively. Optimized formulation showed sustained drug release at the end of 11th hour compared to other formulations. Based on release kinetic model, the drug release data fit well to higuchi model (r2 = 0.9935) indicating the diffusion limited drug release from nanoparticles. Drug release mechanism according to Korsmeyer-Peppas model was found anomalous transport (n = 0.5847). Scanning electron microscopy revealed that the nanoparticles were spherical in shape and there was no crystallization of drug and other excipients....
Zaltoprofen (ZPF) is a non steroidal anti inflammatory analgesic which has excellent effect in rheumatoid arthritis. It shows excellent GI safety as compare to other NSAIDs. Colon targeting drug delivery system specifically delivering drug to the colon, many advantages like improving safety and reducing toxicity when treating local or systemic chronic diseases. To formulate and evaluate colon targeting drug delivery system for the better treatment of rheumatoid arthritis. To study the effect of different hydrogel plug polymers on in-vitro release of ZPF from colon targeting capsule. To carry out stability study of the selected formulation. It may increase bioavailability of the drug. Identification of drug was done by using various testing method. Compatibility studies of drug and polymer were performed by FTIR spectroscopy and DSC. The microcapsule of ZPF was prepared by using different ratios of ZPF and Eudragit S100 and emulsification-solvent evaporation as a method of preparation. FTIR spectroscopy and DSC study revealed that there were no possible interaction between drug and excipients. Microcapsules batch A2 was optimized batch having higher flow property, drug entrapment and % drug release were found and follows Korsmeyer-Peppas model....
The controlled release formulations like solid dosage forms, semi-solid dosage forms, and topical preparations have more importance in pharmaceutical industry due to their efficacy and patient compliance. The topical preparations are supposed to work on the surface of the skin. After application on skin these formulation releases their active ingredient and causes the accumulation of active ingredient which is quickly absorbed. This accumulation causes irritation of skin and high concentration of actives in the circulation. Thus, the microsponge delivery system is an approach to increase the amount of time that an active ingredient remains present either on skin or within the epidermis, which minimizes the transdermal penetration of drug. Microsponges are micro-porous polymeric bead which are loaded with an active ingredient. This system can be incorporated in dosage forms such as creams, lotions, ointments, gels, powders and recently in tablets....
The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Several polymeric systems have been used to fabricate ocuserts for better ocular drug delivery and increased retention of drug, in which ocuserts have shown advantages to overcome the disadvantages of conventional dosage forms. Moxifloxacin is a novel fourth generation fluoroquinolone antibacterial drug effective in the treatment of bacterial conjunctivitis. Ocuserts containing different combination of HPMC (E- 50), EC and PVP (K-30). The ocuserts were prepared by solvent casting technique and characteristic like thickness, weight variation, drug content, moisture loss, moisture absorption, ocular irritation study, in vitro release sterility test and microbiological studies. All the ocuserts were found to be sterile, non irritant and stable. The drug content of the ocuserts was found to be varied between 96.00 - 97.90%. All the formulations followed zero order release pattern. Ocusert (MHF 4) containing EC (600 mg) and HPMC (400 mg) has shown good in-vitro controlled release i.e. 77.13% was found to be better than the other formulations over an extended period of 8 hours and showed excellent microbiological activity for 3 days and remained stable and intact at ambient conditions....
Lipid nanoparticles (LN) have gained immense attention these days as they avail the combined benefits of both lipids and nano sized particles. LN’s are considered to be a safer alternative to polymeric nanoparticles owing to their biodegradable and biocompatible nature. Thus the Lipid nanoparticles are preferred for oral administration of drugs with poor solubility and low bioavailability. The present work gives a detailed description of the nanostructured lipid carriers (NLC), their characteristics and types, mechanism of oral absorption and advantages. The various methods used for the preparation of NLC are briefly described. It also includes their characterization by means of particle size and zeta potential measurement, determination of entrapment efficiency, TEM analysis, DSC and XRD study, in-vitro – ex-vivo studies and stability study. Lyophilization process is also described as a means of stability enhancement and the characterization of lyophilized product is also included....
Nanotechnology is the manipulation and use of materials and devices at the scale of atoms and molecules. This is the scale at which the basic functions of the biological world operate and materials of this size display unusual physical and chemical properties which are attributed to an increase in surface area compared to volume as particles get smaller and also to the grip of weird quantum effects at the atomic scale. Nanotechnology is a rapidly expanding area of research with huge potential in many sectors, ranging from healthcare to electronics. In medicine, it promises to revolutionize drug delivery, gene therapy, diagnostics, and many areas of research, development and clinical application. Nanotechnology will sure change the present scenario of the science and technology completely. Futuristic view of nanotechnology in the field of veterinary sciences is more focused in the present review. The role of nanotechnology in diagnosis, treatment, animal nutrition and veterinary public health were discussed....
Now-a-days the applications of nanotechnology and nanomaterial’s can be found in many topical preparations. Topical preparations are used for the localized effects at the site of their application by virtue of drug penetration into the underlying layers of skin or mucous membranes. Topical delivery can be defined as the application of a drug containing formulation to the skin to directly treat cutaneous disorders (e.g. acne) or the cutaneous manifestations of a general disease (e.g. fungal infections) with the intent of containing the pharmacological or other effect of the drug to the surface of the skin or within the skin in this review we discuss structure of skin, skin diseases and different polymeric nanoparticles use for the topical drug delivery....
Topical treatment of skin diseases is favourable due to the lower risk of systemic side effects. But however the presence of epidermal lipids on stratum corneum prevents the penetration of actives into the viable skin. Solid lipid nanoparticles (SLN) may be considered as an option for topical treatment of skin diseases. Due to its small particle size, SLN results into the formation of occlusive film on the skin surface. These results into targeted drug delivery, controlled release of actives and occlusion associated with improved skin penetration and skin hydration which makes SLN favourable for topical treatment of skin diseases. Here in this review we mention the potential of SLN in treatment of various skin diseases....
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