Novel expandable gastro retentive system by unfolding mechanism of levetiracetam using simple lattice design – Formulation optimization and in vitro evaluation

Srinivasan, S.; Karthikeyan, E.; Chandana, P.J.

doi:10.1016/j.bfopcu.2017.02.003

Cited by 24 publications

(21 citation statements)

References 14 publications

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“…Optimization of Drug Loaded Middle Layer of GRSP: Lower and upper backing layers were not considered for optimization as they were used only for decreasing the initial bursting effect. The drugloaded polymeric film was optimized for folding endurance, drug release, mucoadhesion, tensile strength, integrity, and sustained release of drug till 12 h without bursting effect as described below 1,6,16 .…”

Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

“…The polynomial equations can be used to draw conclusions after considering the magnitude of the coefficient and the mathematical sign it carries (i.e., positive or negative). Film Thickness: Film thickness was measured using by digital screw gauge (Digital micrometer, Mitutoyo, Japan) at three different places and then mean ± SD values were calculated 1,2,15,18,19 .…”

Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

“…Mucoadhesive Force: Mucoadhesion of GRSP of the metronidazole to the stomach was determined to check their ability to stick to gastric mucosa using double beam physical balance in triplicate 1,6,16 . The stomach mucosa of goat used was obtained from a local slaughterhouse washed with ringer solution and was kept in simulated saliva fluid with a pH of 6.8 at 4 ºC till use.…”

Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

“…In-vitro Dissolution Studies: In-vitro dissolution studies are carried out in triplicate using GRSP of 5 cm × 3 cm containing metronidazole 250 mg and USP type I (Basket type) dissolution apparatus 1,2,6,7 . The dissolution study was carried out at 75 RPM using 900 ml 0.1N HCl (pH 1.2) as a dissolution medium.…”

Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

“…A number of approaches for gastroretentive dosage form (GRDF) have been designed like 1) Floating drug delivery system (low-density drug delivery system), 2) Mucoadhesive drug delivery system 3) Expandable drug delivery system like super porous hydrogels 4) High-density drug delivery system 5) Incorporation of Passage Delaying Food Agents, etc. 4,5,6 An alternative strategy is to combine bioadhesion with the ability to expand by unfolding and swelling using levetiracetam initiated by S Sivaneswari et al 1 Gastro retentive drug-loaded polymeric films were also previously investigated and the effect of shape, folding pattern and polymer characteristics on gastric retention has been studied. D Sathish et al, Developed bilayer drugloaded expandable film of furosemide 2 .…”

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The aim of the present research was to develop and optimize novel expandable gastro retentive formulation of metronidazole to give local action for the management of Helicobacter pylori infection. The formulation contained a drug-loaded sandwich patch prepared by solvent casting method folded into a hard gelatin capsule. Metronidazole being needle shape crystals soluble in 0.1 N HCl, but after drying, the formulation show bursting effect in first 1 h. To avoid this drug-loaded middle layer containing Xanthan gum and HPMC E15 as release retardants was sandwiched between baking layers of HPMC E15. Drug loaded middle layer was subjected to 3 2 full factorial design with concentration of HPMC E15 (X 1) and Xanthan gum (X 2) as independent variables and release of the metronidazole at 1 st h and at 4 th h as Responses. According to 3 2 full factorial design 9 batches were prepared and evaluated for thickness, folding endurance, mucoadhesion, drug content and % drug release. The thickness of formulations F1 to F6 was found to be in the range of 0.266 to 0.352 mm. Folding endurance, Mucoadhesion, and % of drug content of F1-F9 were found to be between 100 to 250, 2.2 to 4.2 N and 98.35% to 99.65% respectively. In-vitro drug release of F1-F9 batches showed bursting effect in F1-F4 batches while optimized batch F6 showed 99.89% release in 12 h. HPMC E15: Xanthan gum with 1.5%: 0.8% concentration (F6) was found to be optimized with good folding-endurance, mucoadhesion, and sustained release till 12 h. INTRODUCTION: Oral drug delivery is the most preferred route of administration due to ease of administration, patient compliance, and flexibility in formulation 1, 2. From last few decades number of oral sustained release dosage forms has been developed due to their considerable therapeutic advantages over conventional dosage forms 3 .

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Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

Section: Fig 1: Folded Grsp Of Metronidazolementioning

confidence: 99%

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Electrospun nanofibers of poly (lactic acid)/poly (ε‐caprolactone) blend for the controlled release of levetiracetam

Ghafouri

Mousavi

Khakestani

et al. 2022

Polymer Engineering & Sci

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This study deals with poly(lactic acid) (PLA), poly(ε‐caprolactone) (PCL), and their blend electrospun nanofibers (ESNF) as novel systems for the release of levetiracetam (LEV). Scanning electron microscopy demonstrated that the morphology of all samples is smooth and beads‐free. In addition, with increasing LEV content, the average diameters of PLA, PCL, and PCL/PLA ESNF enhanced by almost 69%, 41%, and 14%, respectively. FTIR spectroscopy was utilized to confirm the structure of polymer and drug, polymer‐drug interaction, and the observation of functional groups. The pore percentage was also diminished by adding LEV. The results of x‐ray diffraction revealed that the crystallinity decreased from 18.2%, 40.1%, and 21.5% for PLA, PCL, and PLA/PCL ESNF, respectively, to 15%, 31.2%, and 13.6% for the samples containing 18 wt% LEV. In addition, PLA ESNF containing 10 and 18 wt% LEV demonstrated a steady uptrend for drug release, while PCL and PLA/PCL ESNF containing 10 and 18 wt% LEV initially indicated an abrupt increase in drug release and then became steady. Moreover, drug release kinetics were evaluated using different models such as zero order, first order, Higuchi, and Korsmeyer‐Peppas models and the best model for predicting the drug release behavior was selected.

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