scholarly journals DEVELOPMENT AND EVALUATION OF MUCOADHESIVE NANOGEL OF NEVIRAPINE FOR VAGINAL APPLICATION

2019 ◽  
pp. 144-149
Author(s):  
Sheikh Sofiur Rahman ◽  
ABDUL BAQUEE AHMED
Keyword(s):  
Hiv Infection ◽  
Ex Vivo ◽  
Vaginal Fluid ◽  
Content Uniformity ◽  
Vaginal Mucosa ◽  
Salting Out ◽  
Zero Order Kinetics ◽  
The Stability ◽  
Ph Range

Objectives: The main objective of this study was to develop and evaluate Nevirapine nanoparticle loaded mucoadhesive gel (NVP-Np mucoadhesive gel) for vaginal application for the treatment of HIV infection.  Methods: NVP loaded nanoparticles were prepared by salting out method followed by incorporation in different gel bases to produce NVP-Np mucoadhesive gel The prepared gels were evaluated for their physicochemical parameters, rheological characteristics, mucoadhesion, in-vitro drug release and ex-vivo permeation of drug across porcine vaginal mucosa.  Results: The result of FT-IR and DSC study confirmed the absence of incompatibility of NVP with excipients used in the formulations. The particle size of the prepared NVP-Np was found to be 243.8 ± 3.15 nm, a polydispersity index (PI) of 0.787± 0.002 and zeta potential value -17.12 mV, which revealed the stability of nanoparticles. All the formulations showed good homogeneity, spreadability, physical appearance and content uniformity. The pH of the mucoadhesive gel formulations was in the range of 3.70 ± 0.03 to 4.56 ± 0.02, which lies in the normal pH range of the vaginal fluid.  The cumulative amounts permeated at 6 h were 832.23 ± 63.45 μg/cm2 , 592.13 ± 82.55 μg/cm2 and 941.32 ± 81.10 μg/cm2 from F1(1% Chitosan), F2(1% Carbopol 974P) and F3 (1% HPMC K100M )  respectively. A linear relationship [r2 > 0.9 (0.97 n 0.99)] was observed between the percentage cumulative amount permeated and time, indicating zero order kinetics. Conclusion: In conclusion, NVP-Np mucoadhesive gel was prepared successfully using salting out followed by a homogenization technique for vaginal application of NVP for the prophylaxis of HIV infection.

scholarly journals Olive Oil Based Organogels for Effective Topical Delivery of Fluconazole: In-vitro Antifungal Study

2020 ◽  
pp. 29-36
Author(s):  
Mohammad Muqtader Ahmed ◽  
Farhat Fatima ◽  
Abdul Bari Mohammed
Keyword(s):  
Olive Oil ◽  
Ex Vivo ◽  
Similarity Index ◽  
Ex Vivo Permeation ◽  
Efficient Delivery ◽  
In Vitro Diffusion ◽  
Permeation Studies ◽  
The Stability ◽  
Hot Melt

The objective of the study was to formulate olive oil based organogels for the topical application of fluconazole (FLZ), to ensure the efficient delivery of the drug deeper in to the skin layers. Methods: Nine formulations developed by hot-melt method using olive oil, sorbitan monostearate (SMS) and FLZ. Prepared formulations characterized for macro evaluations, pH, spreadibility, viscosity, gel-sol transition, in-vitro diffusion study. Further optimized formulation evaluated for ex-vivo percutaneous permeation, in-vitro antifungal studies and stability studies by similarity index. Results: The results of evaluated parameters ensure the stability and effectiveness of the prepared olive oil based organogels. In-vitro diffusion studied reflects decrease in drug release with increase in surfactant concentration due to increase in viscosity. Moreover, ex-vivo permeation studies revealed that the permeation of FLZ was enhanced for optimized formulations (F6) as compared to the marketed gel formulation. Further, the optimized formulation exhibits the broad zone of inhibition against fungal strains in comparison to control and marketed product during in-vitro antifungal study. Conclusion: The olive oil based organogels formulation shown the enhanced permeation of FLZ from organogel network structure with good antifungal activity as compared to the marketed formulation. Henceforth, the FLZ organogel formulations could be used topically for the effective treatment of fungal infection.

scholarly journals DEVELOPMENT, EVALUATION, AND CHARACTERIZATION OF LOSARTAN POTASSIUM BUCCAL PATCHES USING JACKFRUIT POLYMER

2019 ◽  
pp. 24-30
Author(s):  
SOJI S ◽  
ARUN JL
Keyword(s):  
Moisture Content ◽  
In Vitro Release ◽  
Stability Study ◽  
Losartan Potassium ◽  
Content Uniformity ◽  
Zero Order Kinetics ◽  
Sink Condition ◽  
Development Evaluation ◽  
Spectroscopy Studies

Objective: The objective was to develop buccal patches of an antihypertensive drug and losartan potassium using jackfruit polymer for sustained buccal delivery. Methods: The patches were prepared by the solvent casting method. Five formulations were developed with varying concentrations of jackfruit polymer. USP type II apparatus was used to perform in-vitro release study under perfect sink condition. Buccal formulations were developed to a satisfactory level in terms of drug release, bioadhesive strength, content uniformity, moisture content, surface pH, thickness, and stability study. Results: From the results obtained F5 was found as best formulation, having appropriate folding endurance greater than 300, moisture content of 1.14±0.03 percentage (%), moisture uptake of 6.21±0.12%, swelling index (62.78%), bioadhesion strength (37.62±0.25 g), and bioadhesion time of 9 h 5 min. Fourier-transform infrared spectroscopy studies have shown no interactions between drug and polymer. All the formulations followed zero-order kinetics. Conclusion: It can be concluded that mucoadhesive buccal patches of losartan potassium using jackfruit polymer are an auspicious dosage form to prolong the release of drug and enhance its poor oral bioavailability.

scholarly journals Candida albicans forms biofilms on the vaginal mucosa

Microbiology ◽  
2010 ◽  
Vol 156 (12) ◽  
pp. 3635-3644 ◽  
Author(s):  
M. M. Harriott ◽  
E. A. Lilly ◽  
T. E. Rodriguez ◽  
P. L. Fidel ◽  
M. C. Noverr
Keyword(s):  
Biofilm Formation ◽  
Ex Vivo ◽  
Microscopic Analysis ◽  
Vaginal Mucosa ◽  
First Time ◽  
Established Role ◽  
Type Strains

Current understanding of resistance and susceptibility to vulvovaginal candidiasis challenges existing paradigms of host defence against fungal infection. While abiotic biofilm formation has a clearly established role during systemic Candida infections, it is not known whether C. albicans forms biofilms on the vaginal mucosa and the possible role of biofilms in disease. In vivo and ex vivo murine vaginitis models were employed to examine biofilm formation by scanning electron and confocal microscopy. C. albicans strains included 3153A (lab strain), DAY185 (parental control strain), and mutants defective in morphogenesis and/or biofilm formation in vitro (efg1/efg1 and bcr1/bcr1). Both 3153A and DAY815 formed biofilms on the vaginal mucosa in vivo and ex vivo as indicated by high fungal burden and microscopic analysis demonstrating typical biofilm architecture and presence of extracellular matrix (ECM) co-localized with the presence of fungi. In contrast, efg1/efg1 and bcr1/bcr1 mutant strains exhibited weak or no biofilm formation/ECM production in both models compared to wild-type strains and complemented mutants despite comparable colonization levels. These data show for the first time that C. albicans forms biofilms in vivo on vaginal epithelium, and that in vivo biotic biofilm formation requires regulators of biofilm formation (BCR1) and morphogenesis (EFG1).

scholarly journals Development and Optimization of Proniosomal Gel Containing Etodolac: In-vitro, Ex-vivo and In-vivo Evaluation

2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
In Vivo Evaluation ◽  
Vesicle Size ◽  
Skin Delivery ◽  
The Stability

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING ORAL FILM OF ANTI-ALLERGIC DRUG

2018 ◽  
Vol 6 (3) ◽  
pp. 5-16 ◽  
Author(s):  
ABRAHAM LINKU ◽  
JOSEPH SIJIMOL
Keyword(s):  
Ex Vivo ◽  
Methyl Cellulose ◽  
Moisture Loss ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Permeation Study ◽  
Weight Variation

The aim of present work was the development of fast dissolving oral film of Loratadine to overcome the limitations of current routes of administration, to provide immediate action and increase the patient compliance. To improve the bioavailability of the drug, fast dissolving oral film were formulated using different grades of Hydroxy Propyl Methyl Cellulose(HPMC) and various plasticizers like Polyethylene Glycol(PEG) 400, glycerol, Propylene glycol(PG) by solvent casting method. The formulated films were evaluated for film thickness, surface pH, folding endurance, weight variation, % moisture loss, exvivo permeation study, tensile strength, % elongation, drug content uniformity, in vitro dissolution studies,in vitro disintegration test and in vivo study. The optimized formulation (F9) containing HPMC E5 and glycerol showed minimum disintegration time (10.5 s), highest in vitrodissolution (92.5%) and satisfactory stability. Ex vivo permeation study of optimized formulation showed a drug release of 80.6% within 10 min. The milk induced leucocytosis inrat proved that fast dissolving oral films of Loratadine produced a faster onset of action compared to the conventional tablets. These findings suggest that fast dissolving oral film of Loratadine could be potentially useful for treatment of allergy where quick onset of action is required.

scholarly journals Ondansetron Hydrochloride in Treating Patients with Cancer and Chronic Nausea Vomiting

2017 ◽  
Vol 1 (2) ◽  
pp. 01-04
Author(s):  
Hye jin
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Extended Period ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Ondansetron Hydrochloride ◽  
Backing Layer ◽  
Carbopol 934P

The objective of this study was to develop effective bioadhesive buccal bilayered tablets comprising of drug containing bioadhesive layer and drug free backing layer, expected to release the drug in unidirection for extended period of time. Tablets of ondansetron HCl were prepared by direct compression method using bioadhesive polymers like Carbopol 934P, Methocel K4M, Methocel K15M and Hydroxy propyl cellulose in different combinations and concentrations with backing layer of ethyl cellulose. Buccal tablets were evaluated by different parameters such as thickness, hardness, weight uniformity, content uniformity, swelling index, surface pH, ex vivo bioadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation, stability studies in human saliva, in vivo mucoadhesive performance studies and FTIR studies. The modified in vitro assembly was used to measure the bioadhesive strength of tablets with fresh porcine buccal mucosa as model tissue. Bioadhesion strength was increased with increase in the concentration of carbopol. The tablets were evaluated for in vitro release in pH 6.6 phosphate buffer for 8 hr in standard dissolution apparatus. In order to improve the permeation of the drug, tauroglycholate (permeation enhancer) added in the optimized formulation at 10mM concentration. In order to determine the mode of release, the data was subjected to Korsmeyer and Peppas diffusion model. The optimized formula followed non-fickian release mechanism with zero order kinetics. Carbopol 934P and HPC in the ratio of 3:1 could be used to design effective and stable buccoadhesive tablets of ondansetron HCl. The present study concludes that buccal delivery of ondansetron HCl tablets can be good way to bypass the first pass metabolism.

scholarly journals FORMULATION AND EVALUATION OF DIAZEPAM-LOADED INTRAVAGINAL ALGINATE BEADS: AN INVESTIGATION STUDY FOR THE TREATMENT OF PELVIC FLOOR DYSFUNCTION

2018 ◽  
Vol 11 (7) ◽  
pp. 97
Author(s):  
Shereen Ahmed Sabry
Keyword(s):  
Particle Size ◽  
Pelvic Floor ◽  
Ex Vivo ◽  
Pelvic Floor Dysfunction ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
Poloxamer 407 ◽  
Vaginal Mucosa ◽  
Sedative Action

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.

Development of Mucoadhesive Buccal Films of Glipizide

1970 ◽  
Vol 1 (2) ◽  
pp. 177-183
Author(s):  
Mona Semalty ◽  
Ajay Semalty ◽  
Ganesh Kumar ◽  
Vijay Juyal
Keyword(s):  
Controlled Release ◽  
Residence Time ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Potential Candidate ◽  
Sodium Carboxymethylcellulose ◽  
Casting Technique ◽  
Buccal Films

For improving bioavailability in controlled release fashion and to circumvent the hepatic first pass effect of glipizide mucoadhesive buccal films of glipizide were prepared by solvent casting technique. Buccal films were prepared using hydroxy propylmethylcellulose, sodium carboxymethylcellulose, carbopol-934P and Eudragit RL-100. Films were evaluated for their weight, thickness, surface pH, swelling index,       in vitro residence time, folding endurance, in vitro release, ex vivo permeation studies and drug content uniformity. The films exhibited controlled release over more than 6 h. From the study it was concluded that the films containing 5 mg glipizide in 4.9 % w/v hydroxy propylmethylcellulose and 1.5 % w/v sodium carboxymethylcellulose exhibited satisfactory swelling, an optimum residence time and promising drug release thus proved to be potential candidate for the development of buccal films for therapeutic use.

Formulation and In vitro Evaluation of Mucoadhesive Buccal Patches of Ondansetron Hydrochloride

2010 ◽  
Vol 3 (1) ◽  
pp. 860-866
Author(s):  
Shayeda ◽  
Sathish Dharani
Keyword(s):  
Moisture Absorption ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Thickness Variation ◽  
Content Uniformity ◽  
Casting Technique ◽  
Weight Variation ◽  
Ondansetron Hydrochloride

The goal of the present investigation was to design and evaluate mucoadhesive buccal patches of Ondansetron Hydrochloride (OND) which is used for nausea and vomiting associated with cancer chemotherapy and radiotherapy. Permeation of OND was calculated ex vivo using porcine buccal membrane. Buccal films were developed by solvent-casting technique using Hydroxy Propyl Methyl Cellulose(HPMC E15) as mucoadhesive polymer. The patches were evaluated for weight variation, thickness variation, surface pH, moisture absorption, in vitro residence time, mechanical properties, in vitro release, ex vivo permeation studies and drug content uniformity. The formulation F3 was found to give the better results and obeys first order kinetics. 

Transmucosal Delivery of Duloxetine Hydrochloride for Prolonged Release: Preparation, in vitro, ex vivo Characteri-zation and in vitro-ex vivo Correlation

2018 ◽  
Vol 11 (5) ◽  
pp. 4249-4258
Author(s):  
Nagaraj Banala ◽  
Himabindu Peddapalli ◽  
Narendar Dudhipala ◽  
Krishna Mohan Chinnala
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Content Uniformity ◽  
Prolonged Release ◽  
Duloxetine Hydrochloride ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Buccal Tablets ◽  
Transmucosal Delivery

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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