Current Issue : January - March Volume : 2011 Issue Number : 1 Articles : 11 Articles
Oral ingestion has long been the most convenient and commonly employed route of drug delivery due to its ease of administration, least aseptic constraints and flexibility in the design of the dosage form. Tablet coating is one of the oldest pharmaceutical processes; perhaps, in early times the basic purpose of coating had been elegance or organoleptic enhancement, now there are many more reasons to it like environmental protection, taste and odor masking and for better ingestion, product identity and elegance, for putting incompatible components together, gastric protection etc. As this process maintained its status more of an art than a science, it consistently kept offering enough avenues for the pharmaceutical researcher to work on this....
The universal fear of needle sticks is an indicator of the need of convenient and viable alternative modes of vaccine delivery, and to overcome the other problems associated with the conventional injectable vaccines, administering the vaccines through oral route is the best possible approach. But the practice of oral route vaccine delivery is most difficult because of the numerous barriers posed by the gastrointestinal tract. To overcome all the challenges in the design of oral vaccines, many types of antigen carriers were developed from the past two decades, particularly focusing on a specific approach- “by targeting M cells present on Peyer’s Patches”. Current research works carrying on animals and human beings shown that the antigen carriers such as liposomes, emulsions, microparticles, nanoparticles, dendrimers, and niosomes were able to be taken up selectively by M cells on Peyer's patches and the induction of humoral, cellular, mucosal, and systemic immunity was also observed in almost all the cases. This review summarizes recent research efforts of the entire above mentioned novel oral vaccine delivery systems in detail....
To develop nanoparticles for oral controlled release of antifungal drug Clotrimazole and to improve its bioavailability. Nanoparticles of antifungal drug Clotrimazole were prepared by emulsion–solvent evaporation technique using PLGA as polymer. Different formulations were prepared using drug and polymer in 1:1, 1:2, 1:3 ratios respectively. To determine the effect of polymer and PVA the formulations were characterized for their entrapment efficiency, particle size, surface morphology and release behavior. In vivo study was carried out on Laca mice. Plasma drug concentration was determined by validated HPLC technique. The maximum percentage entrapment efficiency was found to be 66.50 ± 1.89. Mean particle size was found to be in the range of 308.0 to 438.5 nm. In vitro drug release studies showed that formulation F1 to F6 followed a diffusion controlled release. The biodistribution data suggested that there was a controlled drug release for 85 (h) with the selected formulations as compared to unencapsulated drug, which was cleared within 4-5 h after intravenous and oral administration. There was a striking improvement in the relative and absolute bioavailability of drug. The oral administration of unencapsulated drug was detected in various body organs such as liver, lungs and spleen up to 6 hrs. In case of drug loaded nanoparticles drug was found in liver, lungs, spleen, small intestine and kidney for one day. It can be concluded that oral administration of Clotrimazole nanoparticles form a sound basis for controlling drug release and improving its bioavailability...
To prepare and evaluate polymeric biodegradable nanoparticles of Etoposide. To overcome the inherent drawback associated with conventional drug delivery of Etoposide, an attempt is being made to design an alternative drug delivery system in form of nanoparticles. By formulating Etoposide in nanoparticles using PLGA, we can reduce toxicity, enhanced therapeutic index and modify pharmacokinetics and tissue distribution. Material and Method: In the present study polymeric biodegradable nanoparticles (NPs) of Etoposide (ETP) were prepared by modified spontaneous emulsification solvent diffusion method using polylactic-co-glycolic acid (PLGA) as biodegradable matrix. The formulations were then characterized with respect to size and its surface morphology, zeta potential, entrapment efficiency, in vitro drug release profile, sterility testing, stability studies and in vivo tissue distribution study. Key findings:The formulated Etoposide-PLGA nanoparticles were spherical with a diameter ranging from 150 to 250 nm. Highest entrapment efficiency was found to be 73.83%. Highest cumulative percent drug release was observed with F-8 (83.50%) in 120 hrs. Formulation F-8 with optimal particle size, high entrapment efficiency and satisfactory in vitro release was selected for in vivo studies. The average targeting efficiency of drug loaded nanoparticles was found to be 27.23±0.126% % of the injected dose in liver, 41.72±0.415% in lungs, 10.63±0.269% % in kidney and 13.24±0.572% in spleen. In conclusion, the drug loaded nanoparticles showed preferential drug targeting to lungs followed by liver, kidney and spleen. Stability studies indicated that 40C is the most suitable temperature for storage of PLGA nanoparticles. Conclusion: Etoposide loaded nanoparticle is endowed with several exclusive advantages and hence holds potential for further research and clinical application....
The objective of the present investigation was to prepare and evaluate an isabgol husk based directly compressible (DC) Adjuvant that can be used as matrixing agent using an agglomeration technique. Addition of hydroxy propyl methylcellulose was found necessary to improve cohesion. Lactose, calcium hydrogen Orthophosphate and Directly compressible vehicle, used along with isabgol in preparation of agglomerates. The agglomerates were evaluated for their flow properties. Tablets were prepared using 95% agglomerates and 5% domperidone, a poorly compressible drug, and were subjected to in vitro drug release study. Out of various formulations (F4) was recognised as an ideal formulation. All the formulations passes the limits....
The aim of the study was to prepare the buccal patches of salbutamol, the bronchodilator having oral bioavailability of 10.8%, using polymers like sodium alginate, carbopol-934P, PVA, and PVP in various proportions while glycerin as a plasticizer. The patches were prepared by solvent casting technique and were subjected to various evaluation parameters like weight uniformity, content uniformity, thickness uniformity, swelling index, folding endurance, surface pH, and in vitro release studies. The Fourier transform infrared spectroscopic studies revealed that there was no interaction between drug and polymers. The viscosities of the polymeric solutions used for formulations were determined using Brookfield viscometer. The tensile strength of the patches was determined using Universal strength testing machine and found satisfactory. In vitro release studies were conducted for drug loaded patches in phosphate buffer solution, pH 6.6. The patches exhibited 48.73 to 102.21% drug release in 45 min. Data of in vitro release from the patches were fit to different equations and kinetic models to explain release profiles. In vitro release followed zero order kinetics. Release of salbutamol from the patches containing sodium alginate followed Higuchi’s model and mechanism was diffusion rate limited. In vivo studies in human volunteers showed 41.88% drug absorption in 30 min from formulation containing sodium alginate. Good correlation among in vitro release and in vivo absorption of salbutamol was observed (R2= 0.986)....
Lamivudine is an antiviral agent used in the treatment of AIDS having moderate half-life of 5-7 hours thus it is a good candidate for the formulation of sustained release dosage forms. In the present work lamivudine loaded chitosan nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP). Nanoparticles of different core: coat ratio were formulated and evaluated for drug content, loading efficiency, particle size, zeta potential, invitro drug release and stability studies. SEM indicated that the nanoparticles were found to be in nanometer range and showed ideal surface morphology. FT-IR studies indicated that their was no chemical interactions between drug and polymer and stability of drug. The invitro release behaviour from all the drug loaded batches were found to follow zero order and provided sustained release over a period of 24 hr. No appreciable difference was observed in the extent of degradation of product during 60 days in which nanoparticles were stored at various temperatures. The developed formulation overcome and alleviates the drawbacks and limitations of lamivudine conventional dosage forms and could possibility be advantageous in terms of increased bioavailability of lamivudine....
The design of effective drug delivery systems has recently become an integral part of the development of new medicines. Gastro retentive drug delivery systems of Aspirin as floating microbeads were prepared with the objective to obtain site specific drug delivery, to extend its duration of action and reduce the side effects. The present study reveals the characterization of Aspirin -loaded agar floating microbead formulations. Six formulations were made depending on the percentage of the SCMC (0.2%, 0.5%, 1.0%, 1.5%, 2.0%, and3.0%). The ionotropic gelation method was used to prepare sodium carboxymethyl cellulose based controlled release agar microbeads of Aspirin. Prepared microbeads were evaluated for particle size analysis, entrapment efficiency, Stability study , Swelling index, buoyancy studies and in vitro drug release Studies . Drug – loading amount, stirring speed, curing time and polymer concentration affects the particle size .The entrapment efficiencies were found in the range of 71.85 ± 2.04 - 94.53 ± 1.02%. The particle sizes were found in the range of 0.82 ± 0.006 - 1.08 ± 0.009 mm. The invitro drug release study showed that the microbeads were prepared using 2 % SCMC had best zero order release and good sustaining effect . The data suggest that Sodium Carboxy methyl cellulose and agar is a potentially useful material for making controlled release Aspirin -loaded floating microbeads by the ionotropic gelation method....
The aim of this work is to formulate a collagen based dermal scaffold containing Glycyrrhiza glabra (Licorice) root extract for the improvement in the quality of wound healing. For this Collagen was isolated from bovine Achilles tendon and tested for its confirmation of presence, purity and sterility. The physicochemical compatibility between collagen and Glycyrrhiza glabra root extract was studied by FT-IR and results obtained suggested no interaction. Collagen based Scaffolds were formulated using different concentrations of Glycyrrhiza glabra root extract 5%w/v, 10%w/v and 15%w/v (GGEICDS- Glycyrrhiza glabra extract incorporated collagen dermal scaffolds). The prepared scaffolds were subjected to physical, biochemical and histopathological examinations. Microshrinkage Temperature of the scaffolds containing 5%w/v,10%w/v & 15%w/v of GGEICDS were found to be 690C, 730C & 780C respectively indicated that they were hydrothermally stable. Wound healing studies on Male Wister Rats were performed for a period of 7 days and it was observed that the 10%w/v GGEICDS treated rats possessed higher amount of hydroxyl proline content 68.9%, when compared to that of the existing Marketed formulation (Neu- skinTM) (59.7%) . Further better wound healing activity was observed in the 10%w/v GGEICDS treated rats (75%) with that of the others including the Marketed formulation (55.2%). When examined histopathologically, more production in the collagen content was clearly observed in 10% w/v GGEICDS treated groups which resulted in the epithelial gap reduction. Further the rise in fibroblast count (62 in 100µ in the wound during the healing process) in 10% GGEICDS treated groups was observed. This research suggested that 10% GGEICDS is a feasible and productive approach in the improvement of dermal wound healing process....
A Mixture design study has been made to evaluate the colonic matrices of okra gum (OG) and Hypromellose using theophylline for combating nocturnal peak symptoms of asthma. As per design fourteen batches of matrices were prepared by wet granulation method and were evaluated for their physicochemical properties. In vitro dissolution was performed in simulated GI fluids viz. pH 1.2 (2h), pH 7.4 (3h), and pH 6.8 (1h) with or without rat caecal contents to check the integrity and release behavior of matrices. Analysis of variance was used to compute the statistical significance of quadratic model of the design. Physicochemical properties of matrices gave satisfactory results and as per I.P. specification. As per ANOVA there were no signs of any problems in our data and data points were almost linear. Formulations with higher amount OG and HPMC showed minimal drug release in upper GIT and were tested further for dissolution in presence of rat caecal contents. It was found that all batches releases its content within 3h of study in presence rat caecal content. These showed colon specific nature of okra gum and might be used as a carrier for chronotherapeutic delivery of theophylline in colon for the treatment of asthma....
Objective: Investigation of a colon specific multiparticulate system based on pH sensitive property and specific enzyme biodegradability was carried out. The basic design consists of pectin microspheres containing Tinidazole and coated with pH sensitive polymer Eudragit S100 so as to maintain the intactness of pectin microspheres till they reach colon. Materials and Methods: The Tinidazole microspheres were prepared in six batches by emulsion dehydration technique using different drug and polymer ratios and coated with Eudragit S100 by solvent evaporation method. Microspheres were evaluated for the particle size, encapsulation efficiency, in vitro release and organ distribution studies. Key findings: In vitro release studies revealed that the release of Tinidazole from the microspheres was mainly influenced by the polymer concentration and maximum release was found in colonic pH due to pH sensitive polymer, Eudragit S100. From the organ distribution studies it was found that the maximum concentration of drug was observed in colon after 6-8h. Conclusion: Eudragit coated pectin microspheres are promising controlled release carriers for colon targeted delivery of Tinidazole....
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