FABRICATION OF BIOADHESIVE OCUSERT WITH DIFFERENT POLYMERS: ONCE A DAY DOSE

Objective: The objective of this current study is to fabricate ocuserts to control the drug release from chosen bioadhesive polymeric matrixes to enhance patient compliance. Ciprofloxacin HCl (CFX HCl) was selected as a model drug.Methods: Different bioadhesive polymers with different film forming capabilities namely Hydroxy Propyl Methyl Cellulose (HPMC K4M), Poly Vinyl Alcohol (PVA), Sodium Carboxy Methyl Cellulose (Na CMC), Hydroxy Propyl Cellulose (HPC), Sodium Alginate (Na Alg.), pullulan and Xanthan Gum (XG) in different ratios were used in fabricating ocuserts using solvent-casting technique. Propylene Glycol (PG) was used as a plasticizer to facilitate the fabrication process. Characterization tests of the developed ocuserts were performed as well as bioadhesive tests and in vitro release studies of the incorporated drug. The obtained results were analysed using different release kinetic models. Stability of the selected ocuserts was investigated at 40±0.5 °C and 75±5% Relative Humidity (RH) for three months’ storage period. In vivo ocular irritation test was performed to investigate the safety of the formula in rabbits’ eyes as well as to test the release profile and thus to estimate In vitro In vivo correlation.Results: All the prepared ocuserts showed the uniformity of film characterization and bioadhesion strength ranged from 240±66 and 158±52dyne/cm2. Selected formula from the in vitro release study tested for in vivo study showed the slow release of ciprofloxacin drug up to 24 h with no signs of eye irritancy. Results for In vitro In vivo correlation showed an excellent correlation with R2 value of 0.9982.Conclusion: PVA based ocuserts proven to be a promising once-daily, effective and safe ocular delivery system of the drug.

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Development of Mucoadhesive Patches for Buccal Administration of Prochlorperazine: Evaluation of In Vitro Release and Mechanical Properties

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/10.37285/ijpsn.2008.1.1.5 ◽

1970 ◽

Vol 1 (1) ◽

pp. 64-70

Author(s):

Chandra Sekhar Kolli ◽

Ramesh Gannu ◽

Vamshi Vishnu Yamsani ◽

Kishan V ◽

Madhsudan Rao Yamsani

Keyword(s):

Mechanical Properties ◽

Drug Release ◽

Moisture Absorption ◽

Release Kinetics ◽

In Vitro Release ◽

Work Of Adhesion ◽

Casting Technique ◽

Vitro Release

The aim of this investigation was to develop and evaluate mucoadhesive buccal patches of prochlorperazine (PCPZ). Permeation of PCPZ was calculated in vitro using porcine buccal membrane. Buccal formulations were developed by solvent-casting technique using hydroxy propylmethyl cellulose (HPMC) as mucoadhesive polymer. The patches were evaluated for in vitro release, moisture absorption and mechanical properties. The optimized formulation, based on in vitro release and moisture absorption studies, was subjected for bioadhesion studies using porcine buccal membrane. In vitro flux of PCPZ was calculated to be 2.14 ± 0.01 µg. h–1.cm–2 and buccal absorption was also demonstrated in vivo in human volunteers. In vitro drug release and moisture absorbed was governed by HPMC content. Increasing concentration of HPMC delayed the drug release. All formulations followed Zero order release kinetics whereas the release pattern was non-Fickian. The mechanical properties, tensile strength (10.28 ± 2.27 kg mm–2 for formulation P3) and elongation at break reveal that the formulations were found to be strong but not brittle. The peak detachment force and work of adhesion for formulation P3 were 0.68 ± 0.15 N and 0.14 ± 0.08 mJ, respectively. The results indicate that suitable bioadhesive buccal patches of PCPZ with desired permeability and suitable mechanical properties could be prepared

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Formulation and Evaluation of Pimozide Buccal Mucoadhesive Patches

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2009.2.4.8 ◽

1970 ◽

Vol 2 (4) ◽

pp. 739-747

Author(s):

Biswajit Basu ◽

Kevin Garala ◽

Thimmasetty J

Keyword(s):

Release Kinetics ◽

In Vitro Release ◽

In Vivo Studies ◽

Poly Vinyl Alcohol ◽

Content Uniformity ◽

In Vivo Absorption ◽

Systemic Drug Delivery ◽

Vitro Release

Within the oral mucosal cavity, the buccal region offers an attractive route of administration for systemic drug delivery. Pimozide patches were prepared using HPMC (15 & 47 cPs), carbopol 934, poly vinyl alcohol, and poly vinyl pyrolidone. FTIR and UV spectroscopic methods revealed that there is no interaction between pimozide and polymers. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH. In vitro release studies of pimozide-loaded patches in phosphate buffer (pH, 6.6) exhibited drug release in the range of 55.32 % to 97.49 % in 60 min. Data of in vitro release from patches were fit in to different equations and kinetic models to explain release kinetics. The models used were zero and first-order equations, Hixon-Crowell, Higuchi and Korsmeyer-Peppas models. In vivo absorption of pimozide from all the patches ranged from 47.96 % to 83.42 % in 60 min in human volunteers. In vivo studies in rabbits showed 85.97% of drug absorption from HPMC-15 cPs patch in 60 min. Good correlation among in vitro release and in vivo absorption of pimozide was observed

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FORMULATION AND EVALUATION OF ANTIFUNGAL NANOGEL FOR TOPICAL DRUG DELIVERY SYSTEM

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2021.v14i10.42436 ◽

2021 ◽

pp. 127-134

Author(s):

ANASUYA PATIL ◽

PRANOTI KONTAMWAR

Keyword(s):

Research Work ◽

In Vitro Release ◽

Gelling Agent ◽

Release Kinetic ◽

Topical Formulation ◽

Ciclopirox Olamine ◽

Carbopol 940 ◽

Vitro Release

Objective: Ciclopirox olamine has been used as antifungal agent. It is used as topical formulation because oral route causes irritation and ulceration of GIT. In this research work, antifungal nanogel formulated to reduce size of particle, improve in-vitro release and in-vivo release. Methods: Ciclopirox olamine nanogel was prepared by homogenization technique and incorporation of gelling agent to produce nanogel. Ciclopirox olamine nanogel formulated using Carbopol 940. Results: Antigungal Nanogels (F1-F6) were subjected to FT-IR analysis and showed no interaction between the drug and excipients. The best formulation (F6) elicited the high in-vitro release of 83.42 % at 8 hours; zeta-potential and particle size, obtained values were 230 nm and -27 mV correspondingly. In-vitro release kinetic models were shown that formulation-F6 follows First-order kinetics and high regression coefficient value r2 0.9866. SEM image of the best formulation-F6 depicts that no breakage of nanogel. The differential scanning calorimetry thermogram of ciclopirox olamine was found to be 140.09.7°C. The DSC thermogram of physical mixture of carbopol 940 and Euragit-S 100 was found to be 1290C and 218 0C. DSC study of nanogel (F6) showed no interaction between drug and excipients. The best formulation-F6 was subjected to in-vivo study on mice which showed better effect in treating dermatitis. Conclusion: It would be concluded that the best formulation-F6 which elicited better in-vitro drug release and enhanced dermatitis scoring. Keywords: Ciclopirox-olamine, Eudragit-S100, Glycerol, Dermatitis, Carbopol-940, Cellophane membrane.

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Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

Thrombosis and Haemostasis ◽

10.1055/s-0038-1651094 ◽

1987 ◽

Vol 57 (02) ◽

pp. 201-204 ◽

Cited By ~ 2

Author(s):

P Y Scarabin ◽

L Strain ◽

C A Ludlam ◽

J Jones ◽

E M Kohner

Keyword(s):

In Vitro Release ◽

Mean Value ◽

Reliable Estimate ◽

Diabetic Patients ◽

Single Measurement ◽

Diabetic Population ◽

The Difference ◽

Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

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Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.1.3 ◽

2017 ◽

Vol 10 (1) ◽

pp. 3582-3593

Author(s):

Chukwuebuka Umeyor ◽

Uchechukwu Nnadozie ◽

Anthony Attama

Keyword(s):

Oral Delivery ◽

In Vitro Release ◽

Carrier System ◽

Solid Lipid ◽

Solid Lipid Microparticles ◽

Release Study ◽

Lipid Microparticles ◽

Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

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Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2013.6.4.10 ◽

2013 ◽

Vol 6 (4) ◽

pp. 2269-2280

Author(s):

Nagratna Dhople ◽

P N Dandag ◽

A P Gadad ◽

C K Pandey ◽

Masthiholimath V S

Keyword(s):

Sustained Release ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Sustained Release Formulation ◽

Prokinetic Drug ◽

Drug Entrapment Efficiency ◽

Itopride Hydrochloride ◽

Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

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Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.4.3 ◽

2012 ◽

Vol 4 (4) ◽

pp. 1537-1543

Author(s):

Sakthikumar T ◽

Rajendran N N ◽

Natarajan R

Keyword(s):

Drug Release ◽

Extended Release ◽

In Vitro Release ◽

Methyl Cellulose ◽

Wet Granulation ◽

Direct Compression ◽

Metoprolol Succinate ◽

Extended Release Formulations ◽

Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension. Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

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