Pub Date : 2010-03-16DOI: 10.5138/IJDD.2010.0975.0215.02017
Sudhir Bhardwaj, V. Jain, R. Jat, A. Mangal, Suman Jain
Fast disintegrating drug delivery system offers a solution for these patients having difficulty in swallowing tablets/ capsules etc. Aceclofenac (anti-inflammatory and analgesic) was selected as the model drug. The poor aqueous solubility of the drug results in variable dissolution rate and hence poor bioavailability. In the present study, an attempt had been made to prepare fast dissolving tablets of the drug using various super disintegrates sodium starch glycolate following by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, disintegration time, water absorption ratio and wetting time, in vitro dissolution studies. All the formulation showed disintegration time in range of 12.2 to 27.5 second along with rapid in vitro dissolution. It was concluded that the fast dissolving tablets of the poor soluble drug can be made by direct compression technique using selective super disintegrantes showing enhanced dissolution, taste masking and hence better patient compliance and effective therapy. Keywords: Aceclofenac; Fast disintegrating; Superdisintegrants; Taste masking
{"title":"Formulation and evaluation of fast dissolving tablet of aceclofenac","authors":"Sudhir Bhardwaj, V. Jain, R. Jat, A. Mangal, Suman Jain","doi":"10.5138/IJDD.2010.0975.0215.02017","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02017","url":null,"abstract":"Fast disintegrating drug delivery system offers a solution for these patients having difficulty in swallowing tablets/ capsules etc. Aceclofenac (anti-inflammatory and analgesic) was selected as the model drug. The poor aqueous solubility of the drug results in variable dissolution rate and hence poor bioavailability. In the present study, an attempt had been made to prepare fast dissolving tablets of the drug using various super disintegrates sodium starch glycolate following by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, disintegration time, water absorption ratio and wetting time, in vitro dissolution studies. All the formulation showed disintegration time in range of 12.2 to 27.5 second along with rapid in vitro dissolution. It was concluded that the fast dissolving tablets of the poor soluble drug can be made by direct compression technique using selective super disintegrantes showing enhanced dissolution, taste masking and hence better patient compliance and effective therapy. Keywords: Aceclofenac; Fast disintegrating; Superdisintegrants; Taste masking","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":"89098972","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.2010.0975.0215.02015
Prashant Khemariya, K. R. Gajbhiye, V. D. Vaidya, R. Jadon, Sachin Mishra, A. Shukla, Mohit Bhargava, S. Singhai, S. Goswami
The aim of the present study was to develop evaluate mouth dissolving tablet of meloxicam. Drug delivery systems became sophisticated as pharmaceutical scientists acquire a better understanding of the physicochemical and biochemical parameters pertinent to their performance. Over the past three decades, mouth dissolving or orally disintegrating tablets have gained considerable attention as a preferred alternative to conventional tablets due to better patient compliance. The most preferrable route of drug administration (e.g. oral) is limited to drug candidate that show poor permeability across the gastric mucosa and those, which are sparingly soluble. A large majority of the new chemical entities and many new existing drug molecules are poorly soluble, thereby limiting their potential uses and increasing the difficulty of formulating bioavailable drug products,so lastlly the purpose of this study was to grow mouth dissolve tablets of Meloxicam. Meloxicam is a newer selective COX-1 inhibitor. These tablets were prepared by wet granulation procedure. The tablets were evaluated for % friability, wetting time and disintegration time. Sublimation of camphor from tablets resulted in better tablets as compared to the tablets prepared from granules that were exposing to vacuum. The systematic formulation approach helped in understanding the effect of formulation processing variables. Keywords: Mouth dissolving tablet; Maloxicam; Bioavailability; NSAID
{"title":"Preparation and evaluation of mouth dissolving tablets of meloxicam","authors":"Prashant Khemariya, K. R. Gajbhiye, V. D. Vaidya, R. Jadon, Sachin Mishra, A. Shukla, Mohit Bhargava, S. Singhai, S. Goswami","doi":"10.5138/IJDD.2010.0975.0215.02015","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02015","url":null,"abstract":"The aim of the present study was to develop evaluate mouth dissolving tablet of meloxicam. Drug delivery systems became sophisticated as pharmaceutical scientists acquire a better understanding of the physicochemical and biochemical parameters pertinent to their performance. Over the past three decades, mouth dissolving or orally disintegrating tablets have gained considerable attention as a preferred alternative to conventional tablets due to better patient compliance. The most preferrable route of drug administration (e.g. oral) is limited to drug candidate that show poor permeability across the gastric mucosa and those, which are sparingly soluble. A large majority of the new chemical entities and many new existing drug molecules are poorly soluble, thereby limiting their potential uses and increasing the difficulty of formulating bioavailable drug products,so lastlly the purpose of this study was to grow mouth dissolve tablets of Meloxicam. Meloxicam is a newer selective COX-1 inhibitor. These tablets were prepared by wet granulation procedure. The tablets were evaluated for % friability, wetting time and disintegration time. Sublimation of camphor from tablets resulted in better tablets as compared to the tablets prepared from granules that were exposing to vacuum. The systematic formulation approach helped in understanding the effect of formulation processing variables. Keywords: Mouth dissolving tablet; Maloxicam; Bioavailability; NSAID","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":"74962468","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.2010.0975.0215.02012
L. Kumar, R. Verma
Nimesulide is a second generation non–steroidal anti–inflammatory agent, which is widely used in the long term therapy of rheumatoid arthritis, in alleviating pain and inflammation. But its short half-life (only 3–4 hr), so its causes more fluctuation. After oral administration Nimesulide causes to produces heart burn, nausea, loose motions, pruritus, etc. The present study based on the preparation of bioadhesive topical gel of Nimesulide, so as to avoid all gastric side effects. For the preparation of bioadhesive topical gel natural polymer aegel marmelos (plant Bale) was used. Bioadhesive polymers are the agents which increases the contact between the formulation and biological membrane, so as to avoid the fluctuation of formulation and behave as a sustained release formulation. In the present study, prepared bioadhesive topical gel was evaluated with the help of different parameters like drug content, spreadability, extrudability, swelling index study, in–vitro drug diffusion study, in-vitro drug release kinetic study and ex–vivo bioadhesive measurement. On the basis of in–vitro drug diffusion study and ex–vivo bioadhesive measurement property of gel, we have concluded that natural polymer aegel marmelos is the best polymer for the preparation of sustained release bioadhesive topical gel. Keywords: Topical gel; Bioadhesion; Natural polymer
{"title":"In vitro evaluation of topical gel prepared using natural polymer","authors":"L. Kumar, R. Verma","doi":"10.5138/IJDD.2010.0975.0215.02012","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02012","url":null,"abstract":"Nimesulide is a second generation non–steroidal anti–inflammatory agent, which is widely used in the long term therapy of rheumatoid arthritis, in alleviating pain and inflammation. But its short half-life (only 3–4 hr), so its causes more fluctuation. After oral administration Nimesulide causes to produces heart burn, nausea, loose motions, pruritus, etc. The present study based on the preparation of bioadhesive topical gel of Nimesulide, so as to avoid all gastric side effects. For the preparation of bioadhesive topical gel natural polymer aegel marmelos (plant Bale) was used. Bioadhesive polymers are the agents which increases the contact between the formulation and biological membrane, so as to avoid the fluctuation of formulation and behave as a sustained release formulation. In the present study, prepared bioadhesive topical gel was evaluated with the help of different parameters like drug content, spreadability, extrudability, swelling index study, in–vitro drug diffusion study, in-vitro drug release kinetic study and ex–vivo bioadhesive measurement. On the basis of in–vitro drug diffusion study and ex–vivo bioadhesive measurement property of gel, we have concluded that natural polymer aegel marmelos is the best polymer for the preparation of sustained release bioadhesive topical gel. Keywords: Topical gel; Bioadhesion; Natural polymer","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":"79933789","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 : 2009-07-05DOI: 10.5138/IJDD.2009.0975.0215.01001
Pragati S, Ashok S, Kuldeep S
Periodontitis, a disease involving supportive structures of the teeth prevails in all groups, ethnicities, races and both genders. The relationship between bacterial plaque and the development of periodontal disease and caries is well established. Antibacterial agents have been used effectively in the management of periodontal infection. The effectiveness of mechanical debridement of plaque and repeated topical and systemic administration of antibacterial agents are limited due to the lack of accessibility to periodontopathic organisms in the periodontal pocket. Systemic administration of drugs leads to therapeutic concentrations at the site of infection, but for short periods of time, forcing repeated dosing for longer periods. Local delivery of antimicrobials has been investigated for the possibility of overcoming the limitations of conventional therapy. The use of sustained release formulations to deliver antibacterials to the site of infection (periodontal pocket) has recently gained interest. These products provide a long-term, effective treatment at the site of infection at much smaller doses. Biodegradable polymers are extensively employed in periodontal drug delivery devices because of their abundant source, lack of toxicity, and high tissue compatibility. A major advantage of natural polymers is that they do not affect periodontal tissue regeneration. Amongst various natural polymers, chitosan, a deacetylated product of chitin is widely used in drug delivery devices. Since it exhibits favourable biological properties such as non-toxicity, biocompatibility, biodegradability and wound healing traits, it has attracted great attention in the pharmaceutical and biomedical fields. The conventional treatment consists of tooth surface mechanical cleaning and root planning, associated or not to the systemic use of high concentrations of antibiotics, but with reduced effectiveness, and adverse effects. The patient compliance to the therapeutic is committed too. In the last decades, the treatment has been optimized for the use of drug delivery systems to the periodontal pocket, with the advantage of delivering the drug in the specific site, sustaining and/or controlling the drug concentration. Recently, the use of new drug delivery systems has been receiving great interest. This review approaches the main delivery systems for the administration of drugs to the periodontal pocket, their usefulness, as well as the advancement of these systems effectiveness in the periodontal therapy. Keywords : Periodontal diseases; Periodontal pocket; Delivery systems; Periodontal pocket delivery
{"title":"Recent advances in periodontal drug delivery systems.","authors":"Pragati S, Ashok S, Kuldeep S","doi":"10.5138/IJDD.2009.0975.0215.01001","DOIUrl":"https://doi.org/10.5138/IJDD.2009.0975.0215.01001","url":null,"abstract":"Periodontitis, a disease involving supportive structures of the teeth prevails in all groups, ethnicities, races and both genders. The relationship between bacterial plaque and the development of periodontal disease and caries is well established. Antibacterial agents have been used effectively in the management of periodontal infection. The effectiveness of mechanical debridement of plaque and repeated topical and systemic administration of antibacterial agents are limited due to the lack of accessibility to periodontopathic organisms in the periodontal pocket. Systemic administration of drugs leads to therapeutic concentrations at the site of infection, but for short periods of time, forcing repeated dosing for longer periods. Local delivery of antimicrobials has been investigated for the possibility of overcoming the limitations of conventional therapy. The use of sustained release formulations to deliver antibacterials to the site of infection (periodontal pocket) has recently gained interest. These products provide a long-term, effective treatment at the site of infection at much smaller doses. Biodegradable polymers are extensively employed in periodontal drug delivery devices because of their abundant source, lack of toxicity, and high tissue compatibility. A major advantage of natural polymers is that they do not affect periodontal tissue regeneration. Amongst various natural polymers, chitosan, a deacetylated product of chitin is widely used in drug delivery devices. Since it exhibits favourable biological properties such as non-toxicity, biocompatibility, biodegradability and wound healing traits, it has attracted great attention in the pharmaceutical and biomedical fields. The conventional treatment consists of tooth surface mechanical cleaning and root planning, associated or not to the systemic use of high concentrations of antibiotics, but with reduced effectiveness, and adverse effects. The patient compliance to the therapeutic is committed too. In the last decades, the treatment has been optimized for the use of drug delivery systems to the periodontal pocket, with the advantage of delivering the drug in the specific site, sustaining and/or controlling the drug concentration. Recently, the use of new drug delivery systems has been receiving great interest. This review approaches the main delivery systems for the administration of drugs to the periodontal pocket, their usefulness, as well as the advancement of these systems effectiveness in the periodontal therapy. Keywords : Periodontal diseases; Periodontal pocket; Delivery systems; Periodontal pocket delivery","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2009-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85496081","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 : 2009-07-05DOI: 10.5138/IJDD.2009.0975.0215.01005
Rakesh Patel, G. Patel, A. Baria
The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems by the solvent evaporation technique by using 15 % w/w of dibutyl phthalate to the polymer weight, incorporated as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Aceclofenac. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations. The results followed the release profile of Aceclofenac followed mixed zero-order and first-order kinetics in different formulation. However, the release profile of the optimized formulation F9 (r2 = 0.9935 for Higuchi) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 1.369 fold enhancements in drug permeation. These results indicate that the formulation containing 15 % of oleic acid with 10 % Isopropyl myristate give better penetration of Aceclofenac through rat skin. Keywords: Aceclofenac, Transdermal Film, Permeation enhancer, In-vitro permeation study.
{"title":"Formulation and evaluation of transdermal patch of Aceclofenac","authors":"Rakesh Patel, G. Patel, A. Baria","doi":"10.5138/IJDD.2009.0975.0215.01005","DOIUrl":"https://doi.org/10.5138/IJDD.2009.0975.0215.01005","url":null,"abstract":"The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems by the solvent evaporation technique by using 15 % w/w of dibutyl phthalate to the polymer weight, incorporated as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Aceclofenac. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations. The results followed the release profile of Aceclofenac followed mixed zero-order and first-order kinetics in different formulation. However, the release profile of the optimized formulation F9 (r2 = 0.9935 for Higuchi) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 1.369 fold enhancements in drug permeation. These results indicate that the formulation containing 15 % of oleic acid with 10 % Isopropyl myristate give better penetration of Aceclofenac through rat skin. Keywords: Aceclofenac, Transdermal Film, Permeation enhancer, In-vitro permeation study.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2009-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90545235","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 : 2009-07-05DOI: 10.5138/IJDD.2009.0975.0215.01003
R. Jadon, Swadesh Nayak, Sabita Amlan, V. D. Vaidya, Prashant Khemariya, Sandip V Sumbhate, S. Nayak
Lornoxicam is a non steroidal anti-inflammatory drug with analgesic properties and belongs to the class oxicams. It is extremely bitter in taste. The purpose of this research was to develop a bitterless oral disintegrating tablet of Lornoxicam. Taste masking was done by complexing Lornoxicam with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratios. In vitro release profile obtained at pH 6.2 indicate that perceivable amount of drug will not be released in saliva while high percentage release (more than 80 % in 30 mins.) would be obtained at acidic pH 1.2 of the stomach. Three super disintegrants were used while preparing the tablets e.g. sodium starch glycolate, crospovidone and crosscarmellose sodium. The tablets were evaluated for different properties like drug content, hardness, friability and disintegration time. The tablets shown good taste and disintegration in oral cavity. Keywords: Oral disintegrating tablet, Lornoxicam, Eudragit EPO, Super disintegrating agents, Taste masking.
{"title":"Taste masking of Lornoxicam by polymer carrier system and formulation of oral disintegrating tablets","authors":"R. Jadon, Swadesh Nayak, Sabita Amlan, V. D. Vaidya, Prashant Khemariya, Sandip V Sumbhate, S. Nayak","doi":"10.5138/IJDD.2009.0975.0215.01003","DOIUrl":"https://doi.org/10.5138/IJDD.2009.0975.0215.01003","url":null,"abstract":"Lornoxicam is a non steroidal anti-inflammatory drug with analgesic properties and belongs to the class oxicams. It is extremely bitter in taste. The purpose of this research was to develop a bitterless oral disintegrating tablet of Lornoxicam. Taste masking was done by complexing Lornoxicam with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratios. In vitro release profile obtained at pH 6.2 indicate that perceivable amount of drug will not be released in saliva while high percentage release (more than 80 % in 30 mins.) would be obtained at acidic pH 1.2 of the stomach. Three super disintegrants were used while preparing the tablets e.g. sodium starch glycolate, crospovidone and crosscarmellose sodium. The tablets were evaluated for different properties like drug content, hardness, friability and disintegration time. The tablets shown good taste and disintegration in oral cavity. Keywords: Oral disintegrating tablet, Lornoxicam, Eudragit EPO, Super disintegrating agents, Taste masking.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2009-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89877415","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 : 2009-07-05DOI: 10.5138/IJDD.2009.0975.0215.01002
M. Singh, D. Singh, S. Saraf
A 32 factorial design was employed to produce oral sustained release lipospheres prepared by modified double emulsion solvent evaporation technique for Serratiopeptidase (acid-labile enzyme) using wax and polar lipid combination as retardants. The effects of formulation variables selected through preliminary trials namely peptide and stabilizer (Tween® 80) concentration was evaluated by F-test on the drug content and size of lipospheres. The results of analysis of variance tests for both effects indicated that the test is significant (p < 0.05). The effect of Tween® 80 concentration (SSY1- 41.66; SSY2 – 25.30) was found to be higher than peptide amount (SSY1- 3.94; SSY2 – 4.03) on the size and drug content of lipospheres. Characterization was carried out through photomicroscopy, scanning electron microscopy, particle size analysis and in vitro drug release study. The effect of formulation variables on the integrity of enzyme was confirmed by in vitro proteolytic activity. The drug release from lipospheres followed first-order kinetics and was characterized by the Higuchi diffusion and Ritger-Peppas model. Lipospheres having maximum drug content (11.93±0.89) released 3-4% enzyme at pH 1.2 in 4 h. In phosphate buffer, lipospheres showed an initial burst release of 20.89±1.87% to 27.89±2.03% in one hour with additional 73.22±2.36% to 94.75±2.78% in next 12 hours. Thus, peptide loaded lipospheres with desirable characters in terms of maximum peptide content and diffusion release pattern were successfully prepared with formulation optimization approach. Keywords: Cetyl alcohol, Enzyme, factorial design, Lipospheres; Peptide, Serratiopeptidase
{"title":"Development and in vitro evaluation of polar lipid based lipospheres for oral delivery of peptide drugs","authors":"M. Singh, D. Singh, S. Saraf","doi":"10.5138/IJDD.2009.0975.0215.01002","DOIUrl":"https://doi.org/10.5138/IJDD.2009.0975.0215.01002","url":null,"abstract":"A 32 factorial design was employed to produce oral sustained release lipospheres prepared by modified double emulsion solvent evaporation technique for Serratiopeptidase (acid-labile enzyme) using wax and polar lipid combination as retardants. The effects of formulation variables selected through preliminary trials namely peptide and stabilizer (Tween® 80) concentration was evaluated by F-test on the drug content and size of lipospheres. The results of analysis of variance tests for both effects indicated that the test is significant (p < 0.05). The effect of Tween® 80 concentration (SSY1- 41.66; SSY2 – 25.30) was found to be higher than peptide amount (SSY1- 3.94; SSY2 – 4.03) on the size and drug content of lipospheres. Characterization was carried out through photomicroscopy, scanning electron microscopy, particle size analysis and in vitro drug release study. The effect of formulation variables on the integrity of enzyme was confirmed by in vitro proteolytic activity. The drug release from lipospheres followed first-order kinetics and was characterized by the Higuchi diffusion and Ritger-Peppas model. Lipospheres having maximum drug content (11.93±0.89) released 3-4% enzyme at pH 1.2 in 4 h. In phosphate buffer, lipospheres showed an initial burst release of 20.89±1.87% to 27.89±2.03% in one hour with additional 73.22±2.36% to 94.75±2.78% in next 12 hours. Thus, peptide loaded lipospheres with desirable characters in terms of maximum peptide content and diffusion release pattern were successfully prepared with formulation optimization approach. Keywords: Cetyl alcohol, Enzyme, factorial design, Lipospheres; Peptide, Serratiopeptidase","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2009-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89851939","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 : 2009-07-05DOI: 10.5138/IJDD.2009.0975.0215.01004
H. Gupta, Aarti Sharma
Vaginal preparations, although generally perceived as safer most , still they are associated with a number of problems, including multiple days of dosing, dripping, leakage and messiness, causing discomfort to users and expulsion due to the self-cleansing action of the vaginal tract. These limitations lead to poor patient compliance and failure of the desired therapeutic effects. For effective vaginal delivery of antimicrobial agents, the drug delivery system should reside at the site of infection for a prolonged period of time. In our present work, we have developed and optimized a chitosan (bioadhesive and permeation enhancer) and gellan gum (ion activated gelling polymer) based in situ gel system of clindamycin for vaginal application. The developed formulation was characterized for various in-vitro parameters e.g. clarity, refractive index, pH, isotonicity, sterility, viscosity, drug release profile, statistical release kinetics, bioadhesive force, retention time, microbial efficacy, irritation test and stability studies. To simulate vaginal conditions, a synthetic membrane (cellophane hydrated with modified simulated vaginal fluid) and sheep vaginal mucosa were used as model membranes. The developed formulation was found to be non irritant, bioadhesive with good retention properties. Developed formulation shows matrix model release kinetic by PCP disso software. The developed formulation is thus a viable alternative to conventional vaginal dosage forms. Keywords: sol-to-gel system; chitosan; gellan gum; vaginal; clindamycin
{"title":"Ion activated bioadhesive in situ gel of clindamycin for vaginal application","authors":"H. Gupta, Aarti Sharma","doi":"10.5138/IJDD.2009.0975.0215.01004","DOIUrl":"https://doi.org/10.5138/IJDD.2009.0975.0215.01004","url":null,"abstract":"Vaginal preparations, although generally perceived as safer most , still they are associated with a number of problems, including multiple days of dosing, dripping, leakage and messiness, causing discomfort to users and expulsion due to the self-cleansing action of the vaginal tract. These limitations lead to poor patient compliance and failure of the desired therapeutic effects. For effective vaginal delivery of antimicrobial agents, the drug delivery system should reside at the site of infection for a prolonged period of time. In our present work, we have developed and optimized a chitosan (bioadhesive and permeation enhancer) and gellan gum (ion activated gelling polymer) based in situ gel system of clindamycin for vaginal application. The developed formulation was characterized for various in-vitro parameters e.g. clarity, refractive index, pH, isotonicity, sterility, viscosity, drug release profile, statistical release kinetics, bioadhesive force, retention time, microbial efficacy, irritation test and stability studies. To simulate vaginal conditions, a synthetic membrane (cellophane hydrated with modified simulated vaginal fluid) and sheep vaginal mucosa were used as model membranes. The developed formulation was found to be non irritant, bioadhesive with good retention properties. Developed formulation shows matrix model release kinetic by PCP disso software. The developed formulation is thus a viable alternative to conventional vaginal dosage forms. Keywords: sol-to-gel system; chitosan; gellan gum; vaginal; clindamycin","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2009-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82733071","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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