Studies on Rebamipide Loaded Gastroretentive Alginate Based Mucoadhesive Beads: Formulation &amp; In-vitro, In-vivo Evaluation

Kashid, Pooja; Doijad, Rajendra; Shete, Amol; Sajane, Sachin; Bhagat, Abhimanyu

doi:10.5530/phm.2016.7.20

Cited by 7 publications

(4 citation statements)

References 5 publications

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“…The increase in the bead size with the increase in the alginate concentration may be ascribed to the increase in the viscosity of the polymer dispersion [26]. These findings were in a good correlation with Kashid et al, who found that there was a significant increase in SA beads size from 0.06±0.02 mm to 0.11±0.014 mm with the increase in the SA amount from 100 mg to 300 mg at 6% CaCl 2 [27].…”

Section: Particle Sizesupporting

confidence: 69%

“…There was a significant increase in the maraviroc alginate microspheres mucoadhesion percentage after 4 h from 55± 3.51 to 78± 2.08 with an increase in the drug to polymer ratio from 1:1 to 1:2, respectively [21]. An increase in the concentration of SA resulted in an increase in the amount of free carboxylic group which was responsible for the binding to the sialic acid group of the vaginal mucosa [27].…”

Section: Swelling Indexmentioning

confidence: 99%

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Formulation and Evaluation of Diazepam-Loaded Intravaginal Alginate Beads: An Investigation Study for the Treatment of Pelvic Floor Dysfunction

Sabry

2018

Asian J Pharm Clin Res

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Objective: The fundamental objective of this research investigation was to develop intravaginal diazepam (DZ)-loaded alginate beads for the management of acute pelvic floor dysfunction (PFD) pain with minimal sedative effect.Methods: DZ loaded beads were prepared by an ionotropic gelation method using SA (sodium alginate) alone, or in combination with either poloxamer 407 (PL), pectin (PC), or xanthan gum (XG) at different ratios in the presence of different concentrations of calcium chloride as a cross-linking agent. The successfully developed beads were evaluated for the particle size, pH, yield percentage, entrapment efficiency, in vitro bioadhesion, swelling percentage, and in vitro drug release. The stability, ex vivo drug permeation, and sedative action of the optimized beads formulations were studied. Results:The particle size of the formulated beads was from 395±3.3 to 515±2.8 µm, yield percentage was from 68.2±1.7 to 87.5±2.1, entrapment efficiency was from 65.6±1.6 to 87.5±2.1. pH ranged from 6.1±0.2 to 6.8±0.6, bioadhesion strength was from 71.5±1.3 to 87.6±3.1, and swelling percentage was in the range from 53.4±3.1 to 85.2±3.7. Approximately 92.4-72.6% of the loaded dose was released from the prepared beads. The optimized beads showed a good stability under the selected storage conditions. About 74.8%, 71.1%, 68.6%, and 63.4% of the loaded dose permeated through the rabbit vaginal mucosa from F7, F9, F3, and F11, respectively. The formulated beads decreased the sedative action associated with orally or parenterally administered DZ. Conclusion:The developed beads were considered a promising candidate to formulate DZ into a new dosage form for the treatment of PFD with a minimum central nervous system sedation.

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Section: Particle Sizesupporting

confidence: 69%

Section: Swelling Indexmentioning

confidence: 99%

Formulation and Evaluation of Diazepam-Loaded Intravaginal Alginate Beads: An Investigation Study for the Treatment of Pelvic Floor Dysfunction

Sabry

2018

Asian J Pharm Clin Res

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“…The FTIR spectra of VerHCl, sodium alginate, VerHCl / sodium alginate physical mixture (1:1 w/w) and VerHCl loaded alginate beads were recorded using (Spectrum Two FTIR spectrometer, Perkin Elmer, USA). The spectra of samples were recorded over the wavelength region of (4000-400 cm −1 ) 21 .…”

Section: Fourier-transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

Statistically-Based Optimization of Verapamil Hydrochloride Loaded Gastroretentive Alginate Beads

Ismail

Raafat²,

Sakran³

2022

Journal of Advanced Pharmacy Research

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Objectives: A gastroretentive drug delivery system is one of many oral drug delivery systems developed to improve drug bioavailability and control drug release. It allows prolongation of drug gastric residence period for several hours. Verapamil Hydrochloride (VerHCl) is a good candidate for gastro retention because it has narrow absorption window and short half life. The goal of this study was formulation and evaluation of optimized VerHCl loaded gastroretentive alginate beads for increasing drug bioavailability and decreasing its dosing frequency. Methods: VerHCl loaded alginate beads were prepared according to 2 3 full factorial design using ionotropic emulsion gelation method. The effect of three formulation variables; oil concentration (%w/v) (X1), polymer concentration (%w/v) (X2) and drug to polymer ratio (X3) was investigated on mean diameter (Y1), drug loading % (Y2), entrapment efficiency (EE%) (Y3), % drug released at 1 (Y4), 5 (Y5) and 8 hr (Y6). The optimized formula was further assessed in terms of in vitro floating, in-vitro drug release, in vivo gastro retention in rats and flowability. Results: Design-Expert® numerical optimization revealed that optimum formulation levels for VerHCl loaded alginate gastroretentive beads were; oil concentration (X1) = 17.2 %w/v, polymer concentration (X2) = 4.34 %w/v and drug to polymer ratio=1.2. The optimized formula exhibited yield% (85.63± 2.65%), Drug loading% (13.60±0.89%), EE% (60.11± 2.52%), prolonged floatability with no initial lag time, sustained in vitro drug release over 8 hr, gastroretention in rats over 8 hr and good flowability. Conclusion: The optimized formula of VerHCl loaded alginate beads could be promising for retaining VerHCl in stomach for a prolonged time which could possibly be advantageous in terms of bioavailability and patient compliance.

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“…The diameter of the microspheres cone will be measured and then the angle of repose. 8,9 tan θ =h/r b. Bulk density (BD) and Tapped density (TD):2 g of granules blend was introduced to a measuring cylinder of 100 ml.…”

Section: Micromeritics Studies Of Prepared Microspheresmentioning

confidence: 99%

Formulation and Characterization of Chitosan Microparticulate System Using Central Composite Design for the Drug: Lafutidine

Kumar¹,

Goyal²

2021

IJPER

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Aim: To formulate a Micro particulate system using central composite design to remain in the stomach for prolonged time and used for Gastroretentive drug delivery. Materials and Methods: Gastroretentive Microspheres were prepared by Emulsion Solvent Evaporation. Micro particulate system were evaluated for micro meritic study, percentage yield, drug entrapment efficiency, in-vitro buoyancy, surface morphology, in-vitro drug release, in-vivo floating study and stability studies. Results: The micro meritic parameters of floating microspheres were found to be within the acceptable limits. The particle size of microspheres was found to be in the range 3.43-15.38 μm. The entrapment efficiency was found to be in the range of 72.02-95.02%. The floating microspheres were spherical in shape with distinct pores, slightly rough surface when observed under scanning electron microscopy. The percentage yield was found to be in the range of 68-89%. The in-vitro buoyancy was found to be in the range of 55.67-92.55% and a total buoyancy time of more than 10 h. The in-vitro dissolution studies showed a cumulative % release in the range of 77.67-95.41%. The optimized formulation F4 was floating in rat stomach for almost 8 h. All the formulations followed Korsemeyer-Peppas kinetics indicating drug release by non-fickian release mechanism. The stability studies showed that floating microspheres were stable at 40 ± 2°C. Conclusion: The optimized formulation showed good floating for 12 h in stomach of rat. The formulation was able to treat the alcohol induced ulcer and also found good stability.

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Studies on Rebamipide Loaded Gastroretentive Alginate Based Mucoadhesive Beads: Formulation & In-vitro, In-vivo Evaluation

Cited by 7 publications

References 5 publications

Formulation and Evaluation of Diazepam-Loaded Intravaginal Alginate Beads: An Investigation Study for the Treatment of Pelvic Floor Dysfunction

Formulation and Evaluation of Diazepam-Loaded Intravaginal Alginate Beads: An Investigation Study for the Treatment of Pelvic Floor Dysfunction

Statistically-Based Optimization of Verapamil Hydrochloride Loaded Gastroretentive Alginate Beads

Formulation and Characterization of Chitosan Microparticulate System Using Central Composite Design for the Drug: Lafutidine

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