The drug which have poor bioavailability it can be administered through parenteral route is regarded the most suitable for drug delivery. Parenteral delivery provides quick onset of action even for the drug with narrow therapeutic index, but patient discomfort will be cause due to the maintenance of systemic drug level repeated installation are required. This type of discomfort can be overcome by developing the drug into a system, which improves patient compliance. Injectable in-situ gelling system is one of the types of such system. This biodegradable injectable in-situ gelling drug delivery system offer attractive opportunities for protein (eg: Albumin), Anti-cancer (eg: Melphalan, Cyclophosphamide), NSAIDs (eg: Diclofenac, Indomethacin) drug delivery and may be possibly extend patent life of these drugs. In this article investigate the injectable in-situ gelling system for extended release parenteral drug delivery system and their preparation, mechanism and evaluation are discussed.
N. K. Sanjana* , C. N. Somashekhar , T. Tamizh Mani
Kalanchoe pinnata is a succulent perennial plant which is commonly known as ‘air plant’. The anti-diabetic activity of Kalanchoe pinnataleaf extracts was investigated in alloxan induced diabetic swiss albino mice. A comparison was made between the action of different extracts of K. pinnata and a known antidiabetic drug glibenclamide. Hypoglycemic activity, determination of blood glucose by glucose oxidase method and total cholesterol was performed in experimental diabetic mice. Dose selection was made on the basis of acuteoral toxicity study as per OECD guidelines. K. pinnataethyl acetate extract (500 mg) and aqueous extract(500 mg) blood glucose levels of these extracts on 14th day of the study were 114 and 121 mg/dL. In alloxan-induced model, blood glucose levels of these extracts on 14th day of the study were 355 mg/dL and 98.67 mg/dL in comparison of diabetic control. In blood serum glucose level extracts of ethyl acetate (500 mg) of K. pinnata exhibited 321 mg/dL at initial day and finally the blood serum glucose reduces to 117 mg/dL. Whereas alloxan treated showed a maximum blood serum glucose level of 333, 346 and 367 on 1 st , 7 th and 14 th days respectively. These ethyl acetate and aqueous extracts of K. pinnataalso showed decreased cholesterol levels when compared to alloxan treated diabetic mice. In all these experiments, extracts of K. pinnata proved to be the potential antidiabetic drug.
N. Sunayana, Vinay B. Raghavendra *, M. Uzma, S.T. Girish
In order to develop a controlled delivery of poorly water-soluble Telmisartan using hydrophilic natural gums like xanthan gum [X] and modified guar gum[MGG] as cost-effective, nontoxic, easily available. The granules of Telmisartan were prepared by wet granulation method using a different ratios drug: gum ratios of X, MGG and XMGG. Magnesium stearate and talc were added to the granules before punching because of to improve the flow ability and compressibility of the granules, and to avoid its adhesion to punch and die. The tablets was analysed to determine hardness, friability, % drug content and invitro release study was carried out. The release of Telmisartan from a gelatinous swollen mass, which controls the diffusion of drug molecules through the polymeric material into aqueous medium. The XMGG matrices show precise controlled release than the X and MGG matrices because of burst effect and fast release in case of X and MGG matrices respectively. Matrices with XMGG show zero-order release via swelling and diffusion mechanism. The XMGG matrices lead to more precise result than X and MGG alone by the utilization of synergistic interaction between two biopolymers and uniformity in the hydration layer in dissolution media.
S. Anupama*, C. N. Somashekar, N. K. Sanjana, T. Tamizhmani
Aim: The aim of the present study is to prepare and characterize floating microspheres containing Lopinavir using Sodium alginate as the polymer. Methods: The Lopinavir loaded floating microspheres were prepared by Ionic gelation method. Floating Microspheres of different core: coat ratio were prepared and characterize for process yield, loading efficiency, particle size, zeta potential, in vitro drug release, kinetic studies and stability studies. Results: The prepared floating microspheres were white, free flowing and spherical in shape. The infrared spectra and differential scanning colorimetry thermographs showed stable character of Lopinavir in the drug-loaded floating microspheres and revealed the absence of drug polymer interactions. The floating microspheres have a zeta potential -15.5 mV. The formulation with the initial lopinavir concentration of 0.5 mg/ml provided the highest loading capacity. The in vitro release behavior from all the drug loaded formulation batches were provided sustained release and follow first order over a period of 12 h. No appreciable difference was observed in the extent of degradation of product during 90 days in which floating microspheres were stored at various temperatures. Conclusion: The best-fit release kinetics was achieved with First order followed by Higuchi plot. The release of Lopinavir was influenced by the drug to polymer ratio and particle size and was found to be diffusion controlled. According to the data obtained, this Sodium alginate-based floating microspheres opens new and interesting perspectives as drug carriers for treating the AIDS.
M. Gayathridevi*, J. Adlin Jino Nesalin, T. Tamizh Mani.
Aim: The aim of the present study is to prepare and characterize nanoparticles containing Nevirapine using Eudragit L 100 as the polymer. Methods: The Nevirapine loaded nanoparticles were prepared by Solvent evaporation method. Nanoparticles of different core: coat ratio were prepared and characterize for process yield, loading efficiency, particle size, zeta potential, in vitro drug release, kinetic study and stability study. Results: The organized nanoparticles be spherical in shape. The infrared spectra and differential scanning colorimetry thermographs showed stable character of Nevirapine in the drug-loaded nanoparticles and revealed the absence of drug polymer interactions. The formulation FE-3 registered has best formulation. The Eudragit L100 nanoparticles have a particle diameter ranging approximately 642.4 nm and a zeta potential -9.26 mV. The in vitro release behavior from all the drug loaded batches were found to follow first order and provided sustained release over a period of 12 h. No appreciable difference was observed in the extent of degradation of product during 90 days in which nanoparticles were stored on different temperatures. Conclusion: The best-fit release kinetics be achieved through First order followed by Higuchi plot. The release of Nevirapine was influenced by the drug to particle size and polymer ratio and was Initiate to be diffusion controlled. According to the data obtained, this Eudragit L 100-based nanoparticles opens new and interesting perspectives as drug carriers for treating the AIDS.
C. Rashmi*, J. Adlino Jino Nesalin, T. Tamizh Mani.