scholarly journals FORMULATION DEVELOPMENT AND CHARACTERIZATION OF GELUCIRE BEADS OF ANTIHYPERTENSIVE DRUG FOR FLOATING DRUG DELIVERY SYSTEM USING 32 FACTORIAL DESIGNS

Author(s):  
KHUSHBOO RANKA ◽  
KAMAL S RATHORE

Objective: The aim of this study was to design and to optimize lipid based beads for multiunit floating drug delivery of ramipril. Methods: The beads prepared by melt-solidification method. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of Gelucire (X1) and Tween 20 (X2) as independent variable and the percentage drug release in 1 (Y1), 6 (Y2), and 12 h (Y3) as dependent variable. Gelucire 43/01 has chosen for release retardant and Tween 20 for solubility enhancement and drug loading agent. Results: The results of multiple linear regression analysis indicated that for obtain a floating drug delivery, the optimum concentrations of both the lipid and drug loading agent should be used. The factorial models were used to prepare optimized floating beads and optimized formulations showed controlled release profiles for the extended period of more than 12 h. Conclusion: From the study, it was concluded that beads of Gelucire for sparingly water-soluble drug ramipril can provide controlled release for extended period.

Author(s):  
Kamble Ravindra K. ◽  
Chauhan Chetan S. ◽  
Kamble Priyadarshani R. ◽  
Naruka Pushpendra S.

The main aim of the present work was to develop the microcapsules of tramadol hydrochloride for the oral sustained release drug delivery. Tramadol hydrochloride a BCS class I drug a centrally acting synthetic analgesic was complexed with Indion 254 ion exchange resin. The microcapsules were prepared by encapsulating the prepared resinates by o/o solvent evaporation technique. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of eudragit RS 100 and plasticized PEG 400. The results of multiple linear regression analysis indicated that for obtaining a sustained release drug delivery the optimum concentrations of both the plasticizer and coating solution to be used. The factorial models were used to prepare optimized microcapsules and optimized formulations showed sustained release profiles for the extended period of more than 12 hrs. From the present investigations concluded that resinate microcapsules of highly water soluble drug can provide controlled release of drug for extended period.Key Words: Tramadol hydrochloride, ion exchange resinate, microcapsules, sustained release


Author(s):  
Poovi Ganesan ◽  
N Damodharan

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach Objective: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly water-soluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (2 11)) orthogonal array design by applying computer optimization technique. Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggests that the cause of cell death is primarily from the effect of TMX present in NLCs. Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.


2003 ◽  
Vol 51 (1) ◽  
pp. 15-19 ◽  
Author(s):  
Masako Kajihara ◽  
Toshihiko Sugie ◽  
Hiroo Maeda ◽  
Akihiko Sano ◽  
Keiji Fujioka ◽  
...  

Author(s):  
Gavaskar Basani ◽  
Madhusudan Rao Yamsani ◽  
Ramya Sri Sura

The aim of current work was to grow extended release multiple unit pellets of Tamsulosin Hydrochloride, is an alpha-blocker, used for the healing of the symptoms of a prostate gland condition called BPH (benign prostatic hyperplasia) by extrusion- spheronization (E/S) and solution/suspension layering (S/S) method. In the Extrusion-Spheronization, A ratio of 75:25, 67:33, 64:36 Tamsulosin Hydrochloride and Microcrystalline cellulose were mixed for making drug pellets and extended release (ER) coating was performed in fluidized bed processor (FBP) by solution/suspension layering with Ethyl cellulose (aqueous. dispersion, 4 cps and 7 cps) and Hypromellose (5cps) with different ratios % weight buildups accordingly. In the Solution/suspension layering (S/S) method, Tamsulosin Hydrochloride drug pellets were prepared by layering onto MCC spheres in FBP. These drug pellets were further coated for extended release with HPMC, 5cps and EC, 7cps. In drug coating stage, drug and different binder (Hypromellose, 5 cps) concentrations 8, 10, 12, 14 mg/unit were coated onto the cores for optimization of binder concentration. The weight of MCC spheres were optimized for further formulations. For all the drug coated pellets, ER coating was given with EC, 7cps and HPMC, 5 cps at a coating level of 8% weight by weight. In the extrusion- spheronization (E/S) Optimization of Drug pellets: Among the trials TD3 (Tamsulosin HCl and MCC) showed good mechanical strength with better yield due to increased MCC concentration. Optimization of Extended Release Coating: Optimized TD3 drug pellets were coated with ER coating using water insoluble polymer (Aq.EC 25% dispersion/ EC, 4cps/ EC, 7cps) and water soluble polymer (HPMC, 5cps). Among these polymers, extended release coating was optimized (TD3E14) with the combination of EC, 7cps and HPMC, 5cps at 8% weight build up. In the Solution/Suspension layering: Optimization of binder concentration in drug coating stage: HPMC, 5cps with 12 mg/unit for TF7 was optimized based on %yield. Optimization of MCC spheres in drug coating stage in formulation of ER pellets with different weight drug pellets: The weight of MCC spheres (160, 170, 180, 190 mg/unit) used in the drug coating stage with binder HPMC, 5cps (12 mg/unit). These drug pellets were given with ER coating at 8% weight buildup by using EC, 7cps and HPMC, 5cps. Among these trials, TF7E7 was optimized. Based on the investigations of the present study, conclusions was. formulating low dose, high soluble, BCS class I drug- Tamsulosin Hydrochloride ER formulation by extrusion-spheronization showed flexibility for batch processing and cost effectiveness while solution/suspension layering was process feasible but time consuming due to high drug loading.


Author(s):  
Upasana Yadav ◽  
Angshuman Ray Chowdhuri ◽  
Sumanta Kumar Sahu ◽  
Nuzhat Husain ◽  
Qamar Rehman

  Objective: In this study, we have made an attempt to the developed formulation of nanoparticles (NPs) of telmisartan (TLM) incorporated in carboxymethyl chitosan (CMCS) for the better drug delivery and enhanced bioavailability.Materials and Methods: The NPs size and morphology were investigated by high-resolution transmission electron microscopy and field emission scanning electron microscopy, respectively. The crystal structures and surface functional groups were analyzed using X-ray diffraction pattern, and Fourier transform infrared spectroscopy, respectively.Results: To increase the solubility of TLM by targeted delivery of the drug through polymeric NPs is an alternative efficient, option for increasing the solubility. TLM nanosuspension powders were successfully formulated for dissolution and bioavailability enhancement of the drug. We focused on evaluating the influence of particle size and crystalline state on the in vitro and in vivo performance of TLM.Conclusion: In summary, we have developed a new approach toward the delivery of poorly water-soluble drug TLM by CMCS NPs. The particles having a good drug loading content and drug encapsulation efficiency. The cytotoxicity of the synthesized NPs is also very less.


2010 ◽  
Vol 12 (1) ◽  
pp. 152-164 ◽  
Author(s):  
Saipin Setthacheewakul ◽  
Wichan Kedjinda ◽  
Duangkhae Maneenuan ◽  
Ruedeekorn Wiwattanapatapee

Author(s):  
Vijay Mishra ◽  
Pallavi Nayak ◽  
Manvendra Singh ◽  
Murtaza M. Tambuwala ◽  
Alaa A. Aljabali ◽  
...  

Background: Silver nanoparticles (AgNPs) are one of the most investigated nanostructures in recent years, which gives more challenging and promising qualities in different biomedical applications. The AgNPs synthesized by the green approach provide potential healthcare benefits over chemical approaches, including improvement of tissue restoration, drug delivery, diagnosis, environmentally friendly and a boon to cancer treatment. Objective: In the current scenario, the development of safe and effective drug delivery systems is the utmost concern of formulation development scientists as well as clinicians. Methods: Google, Web of Science, PubMed, portals have been searched for potentially relevant literature to get latest developments and updated information related to different aspects of green synthesized AgNPs along with their biomedical applications especially in the treatment of different types of cancers. Results: The present review highlights the latest published research regarding the different green approaches for the synthesis of AgNPs, their characterization techniques as well as various biomedical applications, particularly in cancer treatment. In this context, environment friendly AgNPs are proving themselves as better candidates in terms of size, drug loading and release efficiency, targeting efficiency, minimal drug-associated side effects, pharmacokinetic profiling, and biocompatibility issues. Conclusion: With continuous efforts by multidisciplinary team approaches, nanotechnology-based AgNPs will shed new light on diagnostics and therapeutics in various disease treatments. However, the toxicity issues of AgNPs needs the greatest attention as unanticipated toxic effects must be ruled out for their diversified applications.


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