scholarly journals Lyophilized Composite Loaded with Meloxicam-Peppermint Oil Nanoemulsion for Periodontal Pain

Polymers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 2317
Author(s):  
Amal M. Sindi ◽  
Khaled M. Hosny ◽  
Waleed S. Alharbi
Keyword(s):  
Ex Vivo ◽  
Medium Chain Triglyceride ◽  
Stability Index ◽  
Pharmacokinetic Studies ◽  
Peppermint Oil ◽  
Disintegration Time ◽  
Conventional Tablet ◽  
Periodontal Inflammation ◽  
Tablet Dosage

Maintaining oral health helps to prevent periodontal inflammation and pain, which can progress into more detrimental issues if left untreated. Meloxicam (MX) is a commonly used analgesic for periodontal pain, but it can have adverse gastrointestinal effects and poor solubility. Therefore, this study aimed to enhance the solubility of MX by developing a self-nanoemulsifying drug delivery system (SNEDDS). Considering the anti-ulcer activity of peppermint oil (PO), it was added in a mixture with medium-chain triglyceride (MCT) to the MX-loaded SNEDDS formulation (MX-PO-SNEDDS). After optimization, MX-PO-SNEDDS exhibited a PO:MCT ratio of 1.78:1, surfactant mixture HLB value of 14, and MX:oil mix ratio of 1:15, a particle size of 47 ± 3 nm, stability index of 85 ± 4%, ex vivo Jss of 4 ± 0.6 μg/cm2min, and ulcer index of 1 ± 0.25 %. Then, orally flash disintegrating lyophilized composites (MX-SNELCs) were prepared using the optimized MX-PO-SNEDDs. Results reveal that MX-SNELCs had a wetting time of 4 ± 1 s and disintegration time of 3 ± 1 s with a high in vitro MX release of 91% by the end of 60 min. The results of pharmacokinetic studies in human volunteers further demonstrated that, compared to a marketed MX tablets, MX-SNELCs provided a higher Cmax, Tmax, and AUC and a relatively greater bioavailability of 152.97 %. The successfully developed MX-SNELCs were found to be a better alternative than the conventional tablet dosage form, thus indicating their potential for further development in a clinically acceptable strategy for managing periodontal pain.

scholarly journals Nose to Brain Delivery of Phenytoin Sodium Loaded Nano Lipid Carriers: Formulation, Drug Release, Permeation and In Vivo Pharmacokinetic Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1640
Author(s):  
Sreeja C. Nair ◽  
Kollencheri Puthenveettil Vinayan ◽  
Sabitha Mangalathillam
Keyword(s):  
Drug Release ◽  
Olfactory Epithelium ◽  
Drug Transport ◽  
Ex Vivo ◽  
Medical Attention ◽  
Pharmacokinetic Studies ◽  
Phenytoin Sodium ◽  
Drug Solution

An acute epileptic seizure is a seizure emergency fatal condition that requires immediate medical attention. IV phenytoin sodium remains the second line therapeutic agent for the immediate treatment of status epilepticus. Phenytoin sodium formulated as nanolipid carriers (NLCs) seems to be promising as an intranasal delivery system for controlling acute seizures. Three different nanosized phenytoin sodium loaded NLCs (<50 nm, 50–100 nm and >100 nm) were prepared by melt emulsification and was further characterised. In vitro drug release studies showed immediate drug release from phenytoin sodium loaded NLCs of <50 nm size, which is highly essential for acute seizure control. The ex vivo permeation study indicated greater permeation from <50 nm sized NLC through the olfactory epithelium compared to thecontrol drug solution. Invivo pharmacokinetic studies revealed higher drug concentration in CSF/brain within 5 min upon intranasal administration of <50 nm sized phenytoin sodium NLCs than the control drug solution and marketed IV phenytoin sodium, indicating direct and rapid nose to brain drug transport through the olfactory epithelium. The study has shown that formulation strategies can enhance olfactory uptake, and phenytoin sodium NLCs of desired particle sizes (<50 nm) offer promising potential for nose to brain direct delivery of phenytoin sodium in treating acute epileptic seizures.

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 OPTIMIZATION OF STATISTICALLY DESIGNED ACECLOFENAC FAST DISSOLVING TABLETS EMPLOYING STARCH GLUTAMATE AS A NOVEL SUPERDISINTEGRANT

2019 ◽  
pp. 77-88
Author(s):  
R. SANTOSH KUMAR ◽  
SAHITHI MUDILI
Keyword(s):  
Drug Release ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Studies ◽  
Disintegration Time ◽  
Short Period ◽  
Dissolution Efficiency

Objective: To optimize aceclofenac fast dissolving tablets employing starch glutamate as novel superdisintegrant by 23factorial design to improve bioavailability and enhance patient compliance. Methods: Starch glutamate was prepared by the esterification process. Starch glutamate physical and micromeritics properties had been evaluated and the prepared starch glutamate was used as a superdisintegrant for the formulation of the fast dissolving tablets of aceclofenac by direct compression method and optimized by employing 23factorial design. The prepared aceclofenac fast dissolving tablets were evaluated for post compression parameters as well as in vitro and in vivo release characteristics. Optimized formulation stability studies were performed at accelerated conditions for 6 mo as per ICH and WHO guidelines. Results: The prepared starch glutamate was amorphous, insoluble in aqueous and organic solvents were tested. Fast dissolving tablets of aceclofenac were formulated by employing starch glutamate as a superdisintegrant showed good tablet properties and showed an increased dissolution efficiency of the drug. Among all the formulations (F1 to F8), the formulation F8 containing 5% concentration of starch glutamate, croscarmellose sodium and, crospovidone as a superdisintegrants showed 99.7±0.15% of drug release within 5 min. Whereas the formulation F2 containing 5% concentration of starch glutamate, drug release characters were comparable to the formulation F8. Optimized formulation F2 attained peak plasma concentration within a short period and showed increased relative bioavailability of the drug. Conclusion: From the physical properties, disintegration time, in vitro dissolution studies and pharmacokinetic studies, it was concluded that fast dissolving tablets of aceclofenac tablets formulated by employing starch glutamate as a superdisintegrant enhanced the dissolution efficiency and improved the bioavailability of the drug as compared to the pure drug and stable.

FORMULATION AND EVALUATION OF FAST DISSOLVING BUCCAL FILMS OF DIMENHYDRINATE

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 34-41
Author(s):  
M. R Andrea ◽  
◽  
P. M. Dandagi ◽  
A. P. Gadad
Keyword(s):  
Mechanical Properties ◽  
Ex Vivo ◽  
Poloxamer 407 ◽  
Solvent Casting ◽  
Stability Studies ◽  
Casting Method ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Buccal Films

The aim of the present study was to develop a fast dissolving buccal film of dimenhydrinate with good mechanical properties and fast disintegration, producing an acceptable taste when placed in the mouth. The formulations were developed by solvent casting method by using HPMC E5 and HPMC E15 as film formers in different concentrations, propylene glycol as plasticizer and Poloxamer 407 as solubiliser. The resultant films were evaluated for various parameters. the films were found to be satisfactory for all the parameters. All formulations released more than 85% of the drug within 15 minutes. Formulation F7 (1% HPMC E5: 1% HPMC E15) was selected as the optimized formulation based upon the least disintegration time (24.3sec), optimum mechanical properties, percentage drug content (94.96%) and in vitro drug release (95.20%). The ex vivo release was found to be acceptable. Stability studies revealed that the formulation was stable on storage for two months.

Polymeric Precipitation Inhibitor Based Supersaturable Self-microemulsifying Drug Delivery System of Canagliflozin: Optimization and Evaluation

2021 ◽  
Vol 18 ◽  
Author(s):  
Dilpreet Singh ◽  
Ashok K. Tiwary ◽  
Tejwant Singh Kang ◽  
Neena Bedi
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Physical Stability ◽  
In Vitro Dissolution ◽  
Titration Calorimetry ◽  
Substrate Affinity ◽  
Pharmacokinetic Studies ◽  
Poloxamer 188 ◽  
P Glycoprotein

Background: The present investigation attempts to optimize Supersaturable lipid based formulation (SS SMEDDS) of Biopharmaceutical Classification System (BCS) class IV drug canagliflozin (CFZ) and evaluating the oral bioavailability of the formulation. Methods: Preliminary screening revealed Poloxamer 188 to most effectively inhibit precipitation of CFZ after dispersion during in vitro supersaturation studies. Box Behnken Design was employed for designing different formulations and various statistical analysis were done out to select an appropriate mathematical model. The optimized formulation (OSS 1) was evaluated for in vitro drug release and ex vivo permeation studies to evaluate drug release and permeation rate. Pharmacokinetic studies have been done according to standard methodologies. Results: The optimized formulation (OSS 1) containing 781.1 mg SS SMEDDS and 2.24 % w/w Poloxamer 188 was developed at a temperature of 60°C which revealed nano-globule size with negligible aggregation. Isothermal titration calorimetry revealed the thermodynamic state of formed microemulsion with negative ∆G. The optimized formulation was observed to possess physical stability under different stress conditions and acceptable drug content.. In vitro dissolution of optimized SS SMEDDS revealed higher dissolution rate of CFZ as compared with native forms of CFZ. The permeability of CFZ from optimized SS SMEDDS across various excised segments of rat intestine was observed to be multifold higher that manifested in 2.05-fold higher Cmax and 5.64-fold higher AUC0-36h following oral administration to Wistar rats. Conclusion: The results could be attributed to substantial lymphatic uptake and P-glycoprotein substrate affinity of CFZ in SS SMEDDS investigated through chylomicron and P-glycoprotein inhibition approach, respectively.

scholarly journals Formulation and Development of Oral Fast-Dissolving Films Loaded with Nanosuspension to Augment Paroxetine Bioavailability: In Vitro Characterization, Ex Vivo Permeation, and Pharmacokinetic Evaluation in Healthy Human Volunteers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1869
Author(s):  
Ahmed Hassen Elshafeey ◽  
Rania Moataz El-Dahmy
Keyword(s):  
Buccal Mucosa ◽  
Water Solubility ◽  
Ex Vivo ◽  
In Vitro Dissolution ◽  
Healthy Human ◽  
Disintegration Time ◽  
Casting Technique ◽  
Ex Vivo Permeation ◽  
Human Volunteers

Paroxetine (PX) is the most potent serotonin reuptake inhibitor utilized in depression and anxiety treatment. It has drawbacks, such as having a very bitter taste, low water solubility, and undergoing extensive first pass metabolism, leading to poor oral bioavailability (<50%). This work aimed to develop and optimize palatable oral fast-dissolving films (OFDFs) loaded with a paroxetine nanosuspension. A PX nanosuspension was prepared to increase the PX solubility and permeability via the buccal mucosa. The OFDFs could increase PX bioavailability due to their rapid dissolution in saliva, without needing water, and the rapid absorption of the loaded drug through the buccal mucosa, thus decreasing the PX metabolism in the liver. OFDFs also offer better convenience to patients with mental illness, as well as pediatric, elderly, and developmentally disabled patients. The PX nanosuspension was characterized by particle size, poly dispersity index, and zeta potential. Twelve OFDFs were formulated using a solvent casting technique. A 22 × 31 full factorial design was applied to choose the optimized OFDF, utilizing Design-Expert® software (Stat-Ease Inc., Minneapolis, MN, USA). The optimized OFDF (F1) had a 3.89 ± 0.19 Mpa tensile strength, 53.08 ± 1.28% elongation%, 8.12 ± 0.13 MPa Young’s modulus, 17.09 ± 1.30 s disintegration time, and 96.02 ± 3.46% PX dissolved after 10 min. This optimized OFDF was subjected to in vitro dissolution, ex vivo permeation, stability, and palatability studies. The permeation study, using chicken buccal pouch, revealed increased drug permeation from the optimized OFDF; with a more than three-fold increase in permeation over the pure drug. The relative bioavailability of the optimized OFDF in comparison with the market tablet was estimated clinically in healthy human volunteers and was found to be 178.43%. These findings confirmed the success of the OFDFs loaded with PX nanosuspension for increasing PX bioavailability.

Formulation and evaluation of raloxifene hydrochloride dry emulsion tablet using solid carrier adsorption technique

2021 ◽  
Author(s):  
Vishal Patel ◽  
Chintankumar Patel ◽  
Brijesh Patel ◽  
Hetal Thakkar
Keyword(s):  
Oral Bioavailability ◽  
In Vitro Release ◽  
Pharmacokinetic Studies ◽  
Disintegration Time ◽  
Water Emulsion ◽  
Solid Carrier ◽  
Weight Variation ◽  
Dry Emulsion ◽  
Raloxifene Hydrochloride

Aim: The present study focused on the development of a dry emulsion tablet of raloxifene hydrochloride (RXF) using a solid carrier adsorption technique to enhance oral bioavailability. Methods: An oil-in-water emulsion was formulated and converted into dry powder using HPMC K4M plus Aerosil 200, then compressed into tablets. Results: The prepared emulsion was evaluated for globule size, drug content and zeta potential. In vitro release study revealed significantly higher release from emulsion. The prepared tablets possessed acceptable hardness, friability, weight variation, disintegration time, thickness, etc. In vivo pharmacokinetic studies indicated a more than sevenfold increase in oral bioavailability. Stability studies indicated good physical and chemical stability of the developed formulation. Conclusion: The authors successfully formulated dry emulsion tablets with enhanced oral bioavailability.

Effect on Drug Release profile of Meclizine Hydrochloride by using various Dissolution Media

2021 ◽  
pp. 191-197
Author(s):  
Rahul Rajge ◽  
Vishal Mahanur ◽  
Mukund Tawar
Keyword(s):  
Drug Release ◽  
Soft Drink ◽  
In Vitro Dissolution ◽  
Distilled Water ◽  
Drug Release Profile ◽  
Acceptance Criteria ◽  
Disintegration Time ◽  
Time Required ◽  
Tablet Dosage

The present work was carried out to study the probable interactions of commonly used beverages on the release characteristics of Meclizine HCl sustained release tablet dosage form. Studies were carried out to evaluate the alterations in disintegration time and in-vitro dissolution profiles of Meclizine HCl from the tablets. All the studies indicated that the time required for disintegration of Meclizine HCl tablets is more with the modified immersion media as compared with that in water. At the end of the study it was revealed that more than 82% of Meclizine HCl from tablets MF1 was released in Distilled Water and other modified dissolution media except Coffee, Aerated Cola Drink, Non-Aerated Soft Drink and hence, the tablets failed the USP acceptance criteria in water and other dissolution modified media. In Coffee, Aerated Cola Drink, Non-Aerated Soft Drink having passed the USP acceptance criteria. All the three brands of Meclizine HCl viz. MF1, MF2 and MF3 failed to comply with the USP criteria for percentage drug release within 8 h in distilled water.

scholarly journals FORMULATION AND OPTIMIZATION OF QUERCETIN LOADED NANOSPONGES TOPICAL GEL: EX VIVO, PHARMACODYNAMIC AND PHARMACOKINETIC STUDIES

2019 ◽  
pp. 156-165
Author(s):  
Y. SARAH SUJITHA ◽  
Y. INDIRA MUZIB
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Diffusion Method ◽  
Pharmacokinetic Studies ◽  
Topical Gel

Objective: Quercetin is therapeutically hampered because of its poor solubility. The present investigation was aimed to prepare quercetin loaded nanosponges topical gel to enhance the solubility and efficacy of the drug. Methods: Quercetin nanosponges were prepared by emulsion solvent diffusion method. Developed nanosponges optimized by particle size, SEM, entrapment efficiency, FT-IR, DSC, P-XRD, In vitro studies. The optimized formulation of nanosponges was loaded into a topical gel and it was characterized by ex-vivo, in vivo Pharmacodynamic and kinetic studies. Results: The particle size and zeta potential of optimized nanosponges were found to be 188.3 nm and-0.1mV. Surface morphology was studied using SEM Analysis which showed tiny sponge-like structure and entrapment efficiency was found to be 96.5 %. In vitro drug release of optimized nanosponges was found to be 98.6% for 7hours. Optimized nanosponges entrapped gel was prepared by using carbopol 934 and hydroxypropyl methylcellulose as gelling agents. The prepared nanogels were homogenous and ex-vivo skin permeation studies of the optimized nanosponges gel was found to be 98.1% for 5 h, quercetin loaded nanosponges has shown higher skin permeation efficiency (18.4µg/cm2±2.1) compared to pure quercetin gel. The pharmacokinetic and pharmacodynamic studies showed that the quercetin loaded nanosponges has shown more effective when compared to marketed formulation. Conclusion: Quercetin loaded nanosponges gel has shown a significant increase in activity (p<0.05) compared to the marketed formulation (Voveran Emulgel).

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