International Journal of Drug Delivery最新文献_第9页

Methoxsalen loaded chitosan coated microemulsion for effective treatment of psoriasis 甲氧沙胺负载壳聚糖包覆微乳液治疗银屑病的疗效研究

International Journal of Drug Delivery Pub Date : 2010-07-23 DOI: 10.5138/IJDD.2010.0975.0215.02025

J. Behera, Raj K. Keservani, A. Yadav, Meenendra Tripathi, A. Chadoker

引用次数: 30

Synthesis and characterization of dextran esters as coating or matrix systems for oral delivery of drugs targeted to the colon 葡聚糖酯的合成和表征作为包衣或基质系统的口服给药到结肠

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02008

M. Beesh, P. Majewska, F. Th.

{"title":"Synthesis and characterization of dextran esters as coating or matrix systems for oral delivery of drugs targeted to the colon","authors":"M. Beesh, P. Majewska, F. Th.","doi":"10.5138/IJDD.2010.0975.0215.02008","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02008","url":null,"abstract":"Different dextran esters with various degrees of substitution (1, 2 and 3) were synthesized by esterification reaction, with three acid anhydrides: acetic anhydride, propionic anhydride, and butyric anhydride, separately. These modified polysaccharides were characterized by FT-IR, 1H NMR and 13C NMR spectroscopies. Enzymatic degradation of biopolymers by dextranase was also studied. The polymers showing the best degradation profiles were chosen to design blended free films in combination with a polymethacrylate (Eudragit® RS 30D) as a sustained release system for targeting to the colon. These free films were evaluated by permeability of theophylline used as tracer in different in vitro media of the gastro intestinal tract, in presence or in absence of dextranase. From these studies, it was concluded that dextran esters having the lower degree of substitution and constituted of short carbohydrate chains showed the best and significant enzymatic degradation and could be used as a promising carrier for specific colon drug delivery system. Keywords: Colon-Specific Drug Delivery; Polysaccharides; Dextran; Dextranase; Dextran esters; Enzymatic Degradation; Eudragit® RS 30D; Sid-by-side diffusion cell","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73072165","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Design and development of microemulsion drug delivery system of atorvastatin and study its intestinal permeability in rats 阿托伐他汀微乳给药系统的设计与研制及大鼠肠道通透性研究

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02014

Surjyanarayan Mandal, S. Mandal, K. Sawant

{"title":"Design and development of microemulsion drug delivery system of atorvastatin and study its intestinal permeability in rats","authors":"Surjyanarayan Mandal, S. Mandal, K. Sawant","doi":"10.5138/IJDD.2010.0975.0215.02014","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02014","url":null,"abstract":"The objective of this study was to design and develop microemulsion drug delivery system of Atorvastatin and to investigate its intestinal transport behavior using the single-pass intestinal perfusion method in rat. Microemulsion drug delivery system of Atorvastatin was prepared by water titration method and optimized formulation was characterized. The permeability behavior of Atorvastatin over three different concentrations (10, 20 and 40 μg/mL) was studied in each isolated region of intestine (i.e. duodenum, jejunum, ileum and colon) of rat by single-pass intestinal perfusion method in rat method at a flow rate of 0.2 ml/min. The concentration of the sample was determined by HPLC and the effective permeability coefficients were calculated. Considering the high correlation of rat permeability coefficient values with those of human, the human intestinal permeability was predicted using the Lawrence compartment absorption and transit model. The intestinal permeability of Atorvastatin in microemulsion, plain drug suspension and marketed formulation was also compared. The particle size and zeta potential of Atorvastatin microemulsion were (18.2±0.3) nm and (–9.19±0.8) mV respectively. There was no significant difference in permeability coefficient in jejunum, duodenum and ileum with same concentration but higher in colon was observed. The permeability coefficient in jejunum at 10 μg/mL was significantly higher than that at 40 μg/mL (p< 0.01). The estimated human intestinal permeability of Atorvastatin for the microemulsion was relatively higher. Based on the above results, it could be concluded that microemulsion formulation could enhance the intestinal permeability of Atorvastatin and thus could be presented as a possible alternative to traditional oral formulations for improving the oral absorption of Atorvastatin. Keywords: Microemulsion;, Zeta potential; Atorvastatin; Single-pass intestinal perfusion (SPIP) method; Compartment absorption and transit model (CAT)","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77575929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 18

Preformulation studies a view to develop fast release solid dosage form 预制剂研究着眼于开发快速释放固体剂型

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02009

R. Sharma, Ezeddin. I. Kolab

{"title":"Preformulation studies a view to develop fast release solid dosage form","authors":"R. Sharma, Ezeddin. I. Kolab","doi":"10.5138/IJDD.2010.0975.0215.02009","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02009","url":null,"abstract":"The purpose of the present investigation was to increase the solubility and dissolution rate of rofecoxib by the preparation of its solid dispersion using Polyethylene glycol 6000 as a hydrophilic carrier in different proportion ranging from 1:2 to 1:12 using solvent evaporation method. Drug polymer interactions were investigated using Fourier transform infrared spectroscopy (FTIR). The solid dispersions prepared were subjected to assay, solubility and in vitro dissolution studies. The obtained results showed that the solubility was increased 5 fold over that of pure rofecoxib with 1:10 ratio of carrier and the dissolution rate considerably enhanced. The drug-to-carrier ratio was the controlling factor for dissolution improvement with maximum dissolution observed with 1:10 solid dispersion. This increase in the dissolution rate was due to improved wettability by the carrier. At higher level (after 1:10 ratio), the negative effect on dissolution appears that may be due to distortion of molecular dispersion structure, which leaves an insoluble drug particle and increased accumulation of carrier molecule in the bulk, to cause a saturation, by which further solubility of rofecoxib is retarded. FTIR spectra revealed no chemical incompatibility between the drug and PEG6000. The optimized 1:10 (RXB: PEG6000) solid dispersion was used in the formulation of tablet using microcrystalline cellulose as superdisintegant by direct compression. The Flowability and compressibility of the blend was found to be fair for compression. The tablet weight was maintained at nearly 180mg. Keywords: Rofecoxib; Polyethylene glycol 6000; solid dispersions; FTIR; solvent method","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86613373","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Drug delivery to eye: Special reference to nanoparticles 眼睛给药:特别提到纳米颗粒

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02007

Swarnali Das, Preeti K. Suresh

{"title":"Drug delivery to eye: Special reference to nanoparticles","authors":"Swarnali Das, Preeti K. Suresh","doi":"10.5138/IJDD.2010.0975.0215.02007","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02007","url":null,"abstract":"Controlled and sustained delivery of ophthalmic drugs continues to remain a major focus area in the field of pharmaceutical drug delivery with the emergence of new, more potent drugs and biological response modifiers that may also have very short biological half-lives. The major objective of clinical therapeutics is to provide and maintain adequate concentration of drugs at the site of action. In ocular drug delivery, the physiological constraints imposed by the protective mechanisms of the eye lead to poor absorption of drugs with very small fractions of the instilled dose penetrating the cornea and reaching the intraocular tissues. The anatomy, physiology, and biochemistry of the eye render this organ highly impervious to foreign substances. A significant challenge to the formulator is to circumvent the protective barriers of the eye without causing permanent tissue damage. Development of newer, more sensitive diagnostic techniques and novel therapeutic agents continue to provide ocular delivery systems with high therapeutic efficacy. Conventional ophthalmic solution, suspension, and ointment dosage forms no longer constitute optimal therapy for these indications. Nanoparticles and nanosuspensions are showing a better application as compare to conventional delivery sysyems. Polymer nanoparticles proposed are reported to be devoid of any irritant effect on cornea, iris, and conjunctiva and thus appear to be a suitable inert carrier for ophthalmic drug delivery. The benefits of having the drug in the form of a nanoparticulate suspension are: reduction in the amount of dose, drug release for a prolonged period of time, higher drug concentrations in the infected tissue, longer residence time of nanoparticles on the cornea surface, reduction systemic toxicity of drug. Keywords: Nanoparticle; polymer; ocular; bioavailability","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81081669","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 38

Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques 利用固体分散技术提高格列齐特的溶出度和生物利用度

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02011

G. Shavi, Averineni Ranjith Kumar, Y. Usha, K. Armugam, O. Ranjan, K. Ginjupalli, S. Pandey, N. Udupa

{"title":"Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques","authors":"G. Shavi, Averineni Ranjith Kumar, Y. Usha, K. Armugam, O. Ranjan, K. Ginjupalli, S. Pandey, N. Udupa","doi":"10.5138/IJDD.2010.0975.0215.02011","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02011","url":null,"abstract":"Gliclazide is practically insoluble in water and its bioavailability is limited by dissolution rate. To enhance the dissolution rate and bioavailability the present study was aimed to formulate solid dispersions using different water soluble polymers such as polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000) using fusion method and polyvinyl pyrrolidone K- 30 (PVP K 30) by solvent evaporation method. The interaction of gliclazide with the hydrophilic polymers was studied by Differential Scanning Calorimetry (DSC), Fourier Transformation-Infrared Spectroscopy (FTIR) and X-Ray diffraction analysis. Solid dispersions were characterized for physicochemical properties like drug content, surface morphology and dissolution studies. Various factors like type of polymer and ratio of the drug to polymer on the solubility and dissolution rate of the drug were also evaluated. Pharmacokinetic studies of optimized formulation were compared with pure drug and marketed formulation in wistar rats. The dissolution of the pure drug and solid dispersion prepared with PVP K 30 (1:1) showed 38.3 + 4.5 % and 95 + 5.2 % release respectively within 30 min. Peak plasma concentration of pure drug, solid dispersion (PVP K 30) and marketed formulation was found to be 8.76 + 2.5, 16.04 + 5.5 and 9.24 + 3.6 μg/ml respectively, from these results it was observed that there is two fold increase in peak plasma concentration compared to pure drug. Solid dispersion is an effective technique in increasing solubility, dissolution rate and bioavailability of the poorly soluble drugs. Keywords: Gliclazide; solubility; solid dispersion; pharmacokinetics; peak plasma concentration; half life","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83816717","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 47

Ethosome for Enhanced Transdermal Drug Delivery of Aceclofenac 增强乙酰氯芬酸经皮给药的酶体

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02016

V. Dave, Dhirendra Kumar, S. Lewis, S. Paliwal

{"title":"Ethosome for Enhanced Transdermal Drug Delivery of Aceclofenac","authors":"V. Dave, Dhirendra Kumar, S. Lewis, S. Paliwal","doi":"10.5138/IJDD.2010.0975.0215.02016","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02016","url":null,"abstract":"The aim of the current investigation is to evaluate the transdermal potential of novel vesicular carrier, ethosomes, bearing aceclofenac, Non-steroidal anti-inflammatory drugs (NSAIDs) agents having limited transdermal permeation. Aceclofenac loaded ethosomal carriers were prepared, optimized and characterized for vesicular shape and surface morphology,(SEM) scanning electronic microscopy, vesicular size, entrapment efficiency, stability, in- vitro release study. The formulation (Etho5) having 3% phospholipids contant and 40% ethanol showing the grater entrapment (93.3%) and optimal average vesicle size of formulation (Etho5) determine by Malvern Zetamaster ZEM & 0.696μm and zeta potential of formulation was -6.74 mV. The formulation (Etho12) having 3% phospholipids contant and 40% isopropyl alcohol showing the grater entrapment (95.7%). stability profile of prepared system assessed for 45 days. The vesicular suspension was kept in sealed vials (10ml) at 4 ± 2oC and at room temperature for 45 days no change is shown in the entrapment efficiency. The optimized ethosomal formulation showed transdermal flux (226.1 μg/cm²/hr) for ethanolic drug solution which is grater then that of isopropyl alcohol solution (159.0 μg/cm²/hr). The result advocates the potential of ethosome formulation to treat rheumatic disease where facilitated penetration of the drug into muscle and synovial fluid is desirable. In light of the data obtained from experimental work we can expect the ethosome formulation to be safe and very efficient as a drug carrier for systemic as well as topical delivery of drug, holding future in effective transdermal delivery. Keywords: Ethosome; Aceclofenac; Phospholipid; Transdermal","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86379225","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 83

Sodium alginate microspheres for extending drug release: formulation and in vitro evaluation 海藻酸钠缓释微球:配方及体外评价

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02013

M. L. Soni, Mukesh Kumar, K. P. Namdeo

{"title":"Sodium alginate microspheres for extending drug release: formulation and in vitro evaluation","authors":"M. L. Soni, Mukesh Kumar, K. P. Namdeo","doi":"10.5138/IJDD.2010.0975.0215.02013","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02013","url":null,"abstract":"In the present study, spherical microspheres of theophylline (TP) using sodium alginate as the hydrophilic carrier were prepared to prolong the release. The shape, surface and size characteristics were determined by scanning electron microscopy. The microspheres were found to be discreet and spherical in shape and had a smoother surface. The mean diameter of seven alginate microspheres formulations were between 7.6 ± 0.52 and 22.35 ±0.31 μm. It was observed that mean particle size of the microspheres increased with an increase in the concentration of polymer. The entrapment efficiency was found to be in the range of 70–93%. Optimized alginate microspheres were found to possess good sphericity, size and adequate entrapment efficiency. The in vitro release studies were carried out in pH progression media (pH 1.2, 2.5, 4.5, 7 and 7.4 solutions). Results indicated that percent drug release decreased with an increased alginate concentration. TP-loaded Alginate microspheres showed extended in vitro drug release thus use of microspheres potentially offers sustained release profile along with improved delivery of TP. Keywords: Extended drug delivery; Sodium alginate; Microspheres; Bronchial asthma","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89804633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 91

Primary and novel approaches for colon targeted drug delivery - A review 结肠靶向给药的主要方法和新方法综述

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02006

G. Tiwari, R. Tiwari, P. Wal, A. Wal, A. Rai

{"title":"Primary and novel approaches for colon targeted drug delivery - A review","authors":"G. Tiwari, R. Tiwari, P. Wal, A. Wal, A. Rai","doi":"10.5138/IJDD.2010.0975.0215.02006","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02006","url":null,"abstract":"The colon is a site where both local and systemic delivery of drugs can take place. Local delivery could, for example, allow topical treatment of inflammatory bowel disease. Treatment could be made more effective if it were possible for drugs to be targeted directly on the colon. Systemic side effects could also be reduced. Colon specific systems might also allow oral administration of peptide and protein drugs, which are normally inactivated in the upper parts of the gastrointestinal tract. Primary approaches for CDDS (Colon Specific Drug Delivery), which includes prodrugs, pH and time dependent systems and microbially triggered drug delivery system achieved limited success and having limitations. Newly developed CDDS, which includes pressure controlled colonic delivery capsules (PCDCS), CODESTM and osmotic controlled drug delivery are unique in terms of achieving in vivo site specificity and feasibility of manufacturing process. This review also focuses on evaluations of CDDS in general. Keywords: Colon drug delivery systems; Primary approaches; Newly developed approaches; evaluation of colon targeted drug delivery systems","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76715069","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 63

Development, evaluation and optimization of extended release buccal tablets prepared using progressive hydration technology 渐进式水化技术口腔缓释片的研制、评价与优化

International Journal of Drug Delivery Pub Date : 2010-03-16 DOI: 10.5138/IJDD.2010.0975.0215.02010

Amit Gupta, R. Gaud, S. Ganga

{"title":"Development, evaluation and optimization of extended release buccal tablets prepared using progressive hydration technology","authors":"Amit Gupta, R. Gaud, S. Ganga","doi":"10.5138/IJDD.2010.0975.0215.02010","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02010","url":null,"abstract":"Extended release Buccoadhesive buccal tablet for delivery of Nisoldipine were developed using Progressive hydration technology. Technology involves Carbopol 972P (CP), Hypromellose K15M (HPMC) and Polycarbophil (PC) in different amounts. Experiments were designed based on 32 full factorial design to explore effects of CP and HPMC on buccoadhesive strength (BAS) and drug release. Both polymers were found to have effect on swelling index, BAS and drug release which was confirmed by level of significance (p < 0.05). Using quadratic terms a linear second order model that describes a twisted plane of responses were also drawn for elucidation of effect of polymers. Three check points were also taken into account to validate the polynomial equation. Results show that polymers drastically change the drug release mechanism which was confirmed by model fitting into dissolution profile. By customizing the formulation by optimizing the ratio of polymers, desired release (90%) was obtained in the sixth hour and good BAS were obtained for batch F10. Keywords: Buccoadhesive; Nisoldipine; Factorial design; Polynomial equation","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77307199","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8