Pub Date : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02025
J. Behera, Raj K. Keservani, A. Yadav, Meenendra Tripathi, A. Chadoker
Methoxsalen has been used for the treatment of psoriasis. In order to develop alternative formulations for the topical administration of methoxsalen, chitosan coated microemulsion were evaluated as delivery vehicle. Microemulsions were prepared using water, soyabean oil. Egg phosphatidylcholine, ethanol and coated with chitosan. They were characterized for shape and surface morphology, droplet size and size distribution, zeta potential, pH and viscosity. The ability of the system to deliver into the skin was evaluated using dialysis membrane and human cadaver skin. The in vitro permeation data showed that the novel system cumulative amount released was 18.75 % lesser than the microemulsion. These studies clearly show that methoxsalen loaded chitosan-coated microemulsion provides control release of methoxsalen with retention on the skin. Therefore may be appropriate vehicle for topical delivery of methoxsalen. Keywords: Microemulsions; Soyabean; Methoxsalen; Chitosan
{"title":"Methoxsalen loaded chitosan coated microemulsion for effective treatment of psoriasis","authors":"J. Behera, Raj K. Keservani, A. Yadav, Meenendra Tripathi, A. Chadoker","doi":"10.5138/IJDD.2010.0975.0215.02025","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02025","url":null,"abstract":"Methoxsalen has been used for the treatment of psoriasis. In order to develop alternative formulations for the topical administration of methoxsalen, chitosan coated microemulsion were evaluated as delivery vehicle. Microemulsions were prepared using water, soyabean oil. Egg phosphatidylcholine, ethanol and coated with chitosan. They were characterized for shape and surface morphology, droplet size and size distribution, zeta potential, pH and viscosity. The ability of the system to deliver into the skin was evaluated using dialysis membrane and human cadaver skin. The in vitro permeation data showed that the novel system cumulative amount released was 18.75 % lesser than the microemulsion. These studies clearly show that methoxsalen loaded chitosan-coated microemulsion provides control release of methoxsalen with retention on the skin. Therefore may be appropriate vehicle for topical delivery of methoxsalen. Keywords: Microemulsions; Soyabean; Methoxsalen; Chitosan","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":"229 1","pages":"159-167"},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80220444","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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02008
M. Beesh, P. Majewska, F. Th.
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
{"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":"1 1","pages":"22-31"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02014
Surjyanarayan Mandal, S. Mandal, K. Sawant
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)
本研究的目的是设计和研制阿托伐他汀微乳给药系统，并采用单次肠道灌注法研究其在大鼠肠道内的转运行为。采用水滴定法制备了阿托伐他汀微乳给药体系，并对其优化配方进行了表征。采用大鼠法单次肠灌注法，以0.2 mL /min的流速，研究了3种不同浓度(10、20和40 μg/mL)下阿托伐他汀在大鼠小肠各离体区域(即十二指肠、空肠、回肠和结肠)的渗透行为。采用高效液相色谱法测定样品的浓度，计算有效渗透系数。考虑到大鼠的肠通透性系数值与人体的肠通透性系数值具有较高的相关性，采用劳伦斯室吸收和转运模型对人体肠通透性进行预测。比较了阿托伐他汀微乳、普通混悬液和市售制剂的肠通透性。阿托伐他汀微乳粒径为(18.2±0.3)nm, zeta电位为(-9.19±0.8)mV。空肠、十二指肠和回肠的渗透性系数差异不显著，但结肠的渗透性系数较高。10 μg/mL时空肠通透系数显著高于40 μg/mL (p< 0.01)。阿托伐他汀微乳对人体肠道渗透率的估计相对较高。综上所述，微乳制剂可增强阿托伐他汀的肠道通透性，可作为传统口服制剂的替代方案，改善阿托伐他汀的口服吸收。关键词:微乳液;Zeta电位;阿托伐他汀;单次肠灌注法;车厢吸收和运输模型
{"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":"4 1","pages":"69-75"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02009
R. Sharma, Ezeddin. I. Kolab
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
{"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":"47 1","pages":"32-36"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02007
Swarnali Das, Preeti K. Suresh
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
{"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":"42 1","pages":"12-21"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02011
G. Shavi, Averineni Ranjith Kumar, Y. Usha, K. Armugam, O. Ranjan, K. Ginjupalli, S. Pandey, N. Udupa
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
格列齐特几乎不溶于水，其生物利用度受溶出率的限制。以聚乙二醇4000 (PEG 4000)、聚乙二醇6000 (PEG 6000)和聚乙烯吡咯烷酮K- 30 (PVP K 30)为原料，采用熔融法制备固体分散体，以提高其溶解速度和生物利用度。采用差示扫描量热法(DSC)、傅里叶变换红外光谱(FTIR)和x射线衍射分析研究了格列齐特与亲水性聚合物的相互作用。研究了固体分散体的理化性质，如药物含量、表面形貌和溶出度。考察了聚合物种类、药物与聚合物的比例等因素对药物溶解度和溶出率的影响。并与纯药及市售制剂在wistar大鼠体内进行了药动学研究。PVP K 30(1:1)制备的纯药和固体分散体在30 min内的释放度分别为38.3 + 4.5%和95 + 5.2%，纯药、固体分散体(PVP K 30)和市售制剂的血药峰浓度分别为8.76 + 2.5、16.04 + 5.5和9.24 + 3.6 μg/ml，与纯药相比，其血药峰浓度提高了2倍。固体分散是提高难溶性药物溶解度、溶出率和生物利用度的有效技术。关键词:格列齐特;溶解度;固体分散;药物动力学;峰值血药浓度;半衰期
{"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":"9 1","pages":"49-57"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02016
V. Dave, Dhirendra Kumar, S. Lewis, S. Paliwal
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
本研究的目的是评估新型囊泡载体，溶酶体，含乙酰氯芬酸，非甾体抗炎药(NSAIDs)药物的透皮渗透有限。制备并优化了乙酰氯芬酸载体载体，并对其进行了囊泡形状、表面形貌、扫描电镜(SEM)、囊泡大小、包封效率、稳定性、体外释放研究。采用Malvern Zetamaster ZEM & 0.696μm测定了磷脂含量为3%、乙醇含量为40%的配方(Etho5)的包封率为93.3%，最佳平均囊泡大小为-6.74 mV, zeta电位为-6.74 mV。含有3%磷脂和40%异丙醇的配方(Etho12)显示出更大的包裹度(95.7%)。对制备的体系进行了45天的稳定性评估。囊泡悬浮液在4±20℃和室温下密封瓶(10ml)保存45天，包封效率无变化。优化后的乙醇溶液的透皮通量为226.1 μg/cm²/hr，大于异丙醇溶液的159.0 μg/cm²/hr。该结果提倡溶酶体制剂治疗风湿性疾病的潜力，其中促进药物渗透到肌肉和滑液是可取的。根据从实验工作中获得的数据，我们可以预期，乙醇体制剂作为药物载体，无论是全身还是局部给药，都是安全高效的，在有效的透皮给药方面具有广阔的前景。关键词:Ethosome;Aceclofenac;磷脂;经皮的
{"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":"12 1","pages":"81-92"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02013
M. L. Soni, Mukesh Kumar, K. P. Namdeo
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
{"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":"1 1","pages":"64-68"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02006
G. Tiwari, R. Tiwari, P. Wal, A. Wal, A. Rai
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
{"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":"1 1","pages":"1-11"},"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}
Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02010
Amit Gupta, R. Gaud, S. Ganga
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
{"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":"42 5 1","pages":"37-48"},"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}
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