Bilayer mucoadhesive buccal films with prolonged release of ciclopirox olamine for the treatment of oral candidiasis: In vitro development, ex vivo permeation testing, pharmacokinetic and efficacy study in rabbits

Duloxetine hydrochloride is a selective serotonin and nor adrenaline reuptake inhibitor. It is used in the treatment of depression, diabetic peripheral neuropathic pain and in moderate to severe stress urinary incontinence in women. However, it undergoes extensive hepatic first-pass metabolism and susceptible to undergo degradation in acidic environment of stomach, which results in the poor bioavailability. The objective of the present study was to develop and evaluate the mucoadhesive buccal tablets (transmucosal delivery) of duloxetine hydrochloride with a goal of to increase the bioavailability and improve the patient compliance. Mucoadhesive buccal tablets were prepared by a wet granulation technique using mucoadhesive polymers like HPMC K4M, Carbopol 934P and PEO WSR 303. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, in vitro bioadhesion and ex vivo permeation studies. The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets AA1, AB3 and AC1 showed prolonged drug release for a period of 6 h with the Higuchi model release profile. Further, ex vivo permeation studies for optimized tablets were conducted and shown enhanced drug permeation. Therefore, these results demonstrated that the optimized buccal formulation of duloxetine hydrochloride enhances the oral bioavailability by delivered through the buccal route.

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MUCOADHESIVE POLYMERIC FILMS OF ACYCLOVIR PRONIOSOMES FOR BUCCAL ADMINISTRATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i1.39657 ◽

2021 ◽

pp. 135-143

Author(s):

DEEKSHA U. SUVARNA ◽

MARINA KOLAND ◽

ANANTH PRABHU ◽

SINDHOOR S. M.

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Entrapment Efficiency ◽

Polymeric Films ◽

Prolonged Release ◽

Mucosal Permeability ◽

In Vitro Drug Release ◽

Ex Vivo Permeation ◽

Span 60

Objective: The aim of the present work was to formulate and evaluate proniosomes of the poorly soluble drug, acyclovir incorporated in mucoadhesive polymeric films for improved buccal mucosal permeability of the drug while achieving prolonged release. Methods: Acyclovir was formulated as proniosomes using Span 60 and cholesterol. The prepared proniosomes were loaded into mucoadhesive polymeric films prepared with varying quantities of carbopol 934P and HPMC K15M. The proniosome incorporated films were evaluated for physicomechanical characters, mucoadhesion, swelling index, drug content, in vitro drug release and ex vivo permeation through porcine buccal mucosa. Results: Hydration of the proniosomes produced spherical vesicles or niosomes, which was confirmed by Scanning Electron Microscopy. The optimized formulation selected on the basis of vesicle size, entrapment efficiency PDI, Zetz potential and in vitro drug release was selected for incorporation into mucoadhesive polymeric films. All the films showed excellent physicomechanical characters. Formulations with higher proportions of carbopol produced slower in vitro drug release. The kinetics of release of drug from all the formulations appeared to be zero-order based on their regression coefficient values. Comparative evaluation of ex vivo permeation from niosomal and non-niosomal films indicated that the former demonstrated improved mucosal permeation and drug release was also sustained for the 8 h period. Conclusion: Mucoadhesive films impregnated with acyclovir loaded proniosomes could be a potential approach for buccal delivery of acyclovir for improving its absorption and bioavailability.

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Improved in vitro Release and ex vivo Permeation of Zotepine as Microemulsion Gel Formulation through Transdermal Application

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2021.14.1.10 ◽

2021 ◽

Vol 14 (1) ◽

pp. 5343-5352

Author(s):

Akhila Keshoju ◽

Dinesh Suram ◽

Chandra Mouli Golla ◽

Nagaraj B

Keyword(s):

Ex Vivo ◽

In Vitro Release ◽

Gelling Agent ◽

Prolonged Release ◽

Rat Skin ◽

Skin Delivery ◽

Ex Vivo Permeation ◽

Vitro Release ◽

Microemulsion Gel

Zotepine is atypical antipsychotic drug with poor oral bioavailability due to first-pass metabolism and poor aqueous solubility. The objective of the current investigation was preparation and ex vivo characterization of Zotepine (ZT) loaded microemulsion (ZT-ME) and microemulsion gel (ZT-MEG) for enhanced transdermal delivery. ZT-ME formulation was prepared with 7.5% oleic acid, 30% w/v of Tween80 and 30%w/v of absolute ethanol as oil, surfactant and cosurfactant, respectively. Optimized ZT-ME formulation was selected and converted to ZT-MEG using carbopol as gelling agent. ZT-ME and ZT-MEG subjected to in vitro release and ex vivo permeation studies through rat skin, comparison with ZT coarse suspension (ZT-CS). ZT-ME formulation showed desirable physicochemical properties and stable with dilution stress. Prepared ZT-MEG formulation has showed better rheological behaviour and good spreadability. ZT-ME and ZT-MEG showed prolonged release compared with ZT-CS formulation over 24 h. ZT-ME and ZT-MEG exhibited 5-folds and 3.5-folds in permeation through rat skin compared with ZT-CS formulation. Overall, ZT-MEG formulation could be considered as an alternative delivery approach for enhanced skin delivery.

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FORMULATION AND EVALUATION OF ACECLOFENAC PRONIOSOME LOADED ORABASE FOR MANAGEMENT OF DENTAL PAIN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i6.29143 ◽

2018 ◽

Vol 10 (6) ◽

pp. 204

Author(s):

G. V. Radha ◽

K Trideva Sastri ◽

P. Prathyusha ◽

P. Bhanu ◽

Jampala Rajkumar

Keyword(s):

Ex Vivo ◽

Entrapment Efficiency ◽

Prolonged Release ◽

Particle Size Range ◽

Sem Images ◽

Ex Vivo Permeation ◽

Main Motive ◽

Permeation Studies ◽

Span 60

Objective: The main motive is to develop proniosomes loaded orabase for enhanced permeation and prolonged release of aceclofenac for oro dental conditions.Methods: Various aceclofenac (ACL) proniosomal gels were formulated employing various surfactants, span 60 was superior and significant for loading into orabase. The formulations were scrutinized for entrapment efficiency, optical microscopy, in vitro diffusion and release studies, mucoadhesive strength, ex-vivo permeation studies and drug-excipient interactions were determined by FTIR spectroscopy.Results: Considering best entrapment efficiency with span 60 (97.60±1.85) and optimum vesicle shape, along with prolonged drug permeation (45% for 24 h) the formulation F(ACL)1 was selected and optimized for loading into orabase. The F(ACL)1 loaded orabase exhibited significant prolonged release over 14 h, and permeation profiles exhibited nearly two-fold increased flux in comparison with control. Good mucoadhesive strength was observed for proniosomal orabase 6370 dynes/cm2. No evidence of incompatibility amongst formulation components from FTIR studies. SEM images revealed the particle size range from 136 µm to 236 µm for proniosomal orabase.Conclusion: Orabase can be an effective carrier for proniosomes with enhanced permeation and prolonged release for oro-dental conditions.

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Formulation and Evaluation of Lignocaine Hydrochloride Proniosomes Loaded Orabase for Dental Anaesthesia

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v11i3-s.4866 ◽

2021 ◽

Vol 11 (3-S) ◽

pp. 27-34

Author(s):

Radha G. V. ◽

GANESH SAI MYNENI ◽

Sunayana N ◽

Soujanya G. V. R. L. ◽

Charan K

Keyword(s):

Ex Vivo ◽

Entrapment Efficiency ◽

Prolonged Release ◽

Particle Size Range ◽

Sem Images ◽

Ex Vivo Permeation ◽

Vesicle Shape ◽

Permeation Studies ◽

Span 80

The aim of this research is to prepare and evaluate lignocaine HCl Proniosomal orabase for enhanced permeation and prolonged dental anaesthesia effect. Objective: Various lignocaine proniosomal gels were formulated employing various surfactants. Methods: The formulations were scrutinized for entrapment efficiency, optical microscopy, in-vitro diffusion and release studies, mucoadhesive strength, ex-vivo permeation studies and drug – excipient interactions were determined by FTIR spectroscopy. Results: span 80 was found to be superior and significant for loading in to orabase. Considering the best entrapment efficiency with span 80 (91.60%) and optimum vesicle shape, along with prolonged drug permeation (33.6% for 24 h) the formulation F4 was selected and optimized for loading into orabase. The formulation F4 loaded orabase exhibited significant prolonged release over 10 h, and permeation profiles exhibited nearly two – fold increased flux in comparison with control. Good mucoadhesive strength was observed for proniosomal orabase 6273dynes/cm2, No evidence of incompatibility amongst formulation components from FTIR studies. SEM images revealed the particle size range from 50 μmt to 100 μmt for proniosomal orabase. Conclusion: Orabase can be an effective carrier for proniosomes with enhanced retention time at the site of application and provide prolonged release for oro-dental conditions. Keywords: lignocaine Hcl, Oro-dental anaesthesia, Proniosomal gel, Orabase, Entrapment efficiency, prolonged release.

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Low lactate culture benefits the in vitro development of preimplantation mammalian embryos

10.26226/morressier.573c1511d462b80296c98393 ◽

2016 ◽

Author(s):

Rebecca Gilbert

Keyword(s):

In Vitro Development ◽

Mammalian Embryos ◽

Vitro Development

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In-vitro development of early preantral ovarian follicles from postpuberal mice in a simplified culture system

Reproductive Immunology and Biology ◽

10.3192/jsirib2003.20.1_1 ◽

2005 ◽

Vol 20 (1) ◽

pp. 1-4

Author(s):

Hidemi Kada

Keyword(s):

Culture System ◽

Ovarian Follicles ◽

In Vitro Development ◽

Vitro Development

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Development and Ex-vivo Evaluation of Topiramate Mucoadhesive Nanoparticles for Intranasal Delivery

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2020.13.6.10 ◽

2020 ◽

Vol 13 (6) ◽

pp. 5250-5255

Author(s):

Ashwin Kumar Tulasi ◽

Anil Goud Kandhula ◽

Ravi Krishna Velupula

Keyword(s):

Particle Size ◽

Nasal Mucosa ◽

Intranasal Administration ◽

Ex Vivo ◽

Chemical Properties ◽

Brain Targeting ◽

Oral Tablet ◽

Promising Alternative ◽

Ex Vivo Permeation

Topiramate is a second-generation antiepileptic drug used in partial, generalized seizures as an oral tablet. Oral route of administration is most convenient but shows delayed absorption. Moreover, in emergency cases, parenteral administration is not possible as it requires medical assistance. Hence, the present study was aimed to develop topiramate mucoadhesive nanoparticles for intranasal administration using ionotropic gelation method. The developed nanoparticles were evaluated for physico-chemical properties like particle size, zeta potential, surface morphology, drug content, entrapment efficiency, in vitro drug release, mucoadhesive strength, and ex vivo permeation studies in excised porcine nasal mucosa. Optimized nanoparticle formulation (T9) was composed oil mucoadhesive agent (Chitosan 1% w/w), cross linking polymer (TPP) and topiramate 275mg, 100mg and 4% respectively. It showed particle size of 350nm, high encapsulation efficacy and strong mucoadhesive strength. In vitro drug diffusion of optimized formulation showed 95.12% release of drug after 180min. Ex-vivo permeation of drug across nasal mucosa was 88.05 % after 180min. Nasocilial toxicity studies showed optimized formulation did not damage the nasal mucosa. Thus, the intranasal administration of topiramate using chitosan can be a promising alternative for brain targeting and the treatment of epilepsy.

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