scholarly journals Diacerein-Loaded Hyaluosomes as a Dual-Function Platform for Osteoarthritis Management via Intra-Articular Injection: In Vitro Characterization and In Vivo Assessment in a Rat Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 765
Author(s):  
Nouran O. Abdelmageed ◽  
Nadia M. Morsi ◽  
Rehab N. Shamma
Keyword(s):  
Hyaluronic Acid ◽  
Cartilage Damage ◽  
Entrapment Efficiency ◽  
Dual Function ◽  
In Vitro Characterization ◽  
Drug Entrapment Efficiency ◽  
Formulation Parameters ◽  
Acid Gel

The application of intra-articular injections in osteoarthritis management has gained great attention lately. In this work, novel intra-articular injectable hyaluronic acid gel-core vesicles (hyaluosomes) loaded with diacerein (DCN), a structural modifying osteoarthritis drug, were developed. A full factorial design was employed to study the effect of different formulation parameters on the drug entrapment efficiency, particle size, and zeta potential. Results showed that the prepared optimized DCN- loaded hyaluosomes were able to achieve high entrapment (90.7%) with a small size (310 nm). The morphology of the optimized hyaluosomes was further examined using TEM, and revealed spherical shaped vesicles with hyaluronic acid in the core. Furthermore, the ability of the prepared DCN-loaded hyaluosomes to improve the in vivo inflammatory condition, and deterioration of cartilage in rats (injected with antigen to induce arthritis) following intra-articular injection was assessed, and revealed superior function on preventing cartilage damage, and inflammation. The inflammatory activity assessed by measuring the rat’s plasma TNF-α and IL-1b levels, revealed significant elevation in the untreated group as compared to the treated groups. The obtained results show that the prepared DCN-loaded hyaluosomes would represent a step forward in the design of novel intra articular injection for management of osteoarthritis.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

scholarly journals Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 465 ◽  
Author(s):  
Eman A. Mazyed ◽  
Abdelaziz E. Abdelaziz
Keyword(s):  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Ocular Delivery ◽  
Ethanol Injection ◽  
In Vitro Characterization ◽  
Span 60 ◽  
In Vivo Characterization

Acetazolamide (ACZ) is a potent carbonic anhydrase inhibitor that is used for the treatment of glaucoma. Its oral administration causes various undesirable side effects. This study aimed to formulate transgelosomes (TGS) for enhancing the ocular delivery of ACZ. ACZ-loaded transfersomes were formulated by the ethanol injection method, using phosphatidylcholine (PC) and different edge activators, including Tween 80, Span 60, and Cremophor RH 40. The effects of the ratio of lipid to surfactant and type of surfactant on % drug released after 8 h (Q8h) and entrapment efficiency (EE%) were investigated by using Design-Expert software. The optimized formula was formulated as TGS, using poloxamers as gelling agents. In vitro and in vivo characterization of ACZ-loaded TGS was performed. According to optimization study, F8 had the highest desirability value and was chosen as the optimized formula for preparing TGS. F8 appeared as spherical elastic nanovesicles with Q8h of 93.01 ± 3.76% and EE% of 84.44 ± 2.82. Compared to a free drug, TGS exhibited more prolonged drug release of 71.28 ± 0.46% after 8 h, higher ex vivo permeation of 66.82 ± 1.11% after 8 h and a significant lowering of intraocular pressure (IOP) for 24 h. Therefore, TGS provided a promising technique for improving the corneal delivery of ACZ.

BOX–BEHNKEN METHOD TO OPTIMIZE LORNOXICAM PRONIOSOMES: PREPARATION, IN VITRO CHARACTERIZATION AND ANALGESIC ACTIVITY

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (06) ◽  
pp. 21-33
Author(s):  
K. Vijaya Sri ◽  
◽  
D. Sandhya ◽  
M. Manchala ◽  
R. S Dashamukhi
Keyword(s):  
Analgesic Effect ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Factors Affecting ◽  
Drug Diffusion ◽  
Percutaneous Permeation ◽  
In Vitro Characterization ◽  
Diffusion Studies ◽  
Drug Entrapment Efficiency

The objective of present investigation was to develop and evaluation of proniosomes as the carrier of lornoxicam for topical delivery. lornoxicam-loaded proniosomes were prepared by coacervation phase separation method. The Box–Behnken design used in this study helped in identifying the factors affecting drug entrapment efficiency and drug diffusion. Proniosomes were evaluated for appearance, pH, viscosity, entrapment efficiency and in vitro drug diffusion studies. The optimized formulations were further evaluated to vesicle size, shape, zeta potential, percutaneous permeation and analgesic effect. The vesicles were found to be unilamellar, spherical in shape. The analgesic effect of lornoxicam proniosomal gel showed better therapeutic activity.

Ibuprofen loaded nano-ethanolic liposomes carbopol gel system: in vitro characterization and anti-inflammatory efficacy assessment in Wistar rats

2018 ◽  
Vol 38 (3) ◽  
pp. 291-298 ◽  
Author(s):  
Atefeh Afshar Moghaddam ◽  
Abdul Ahad ◽  
Mohd. Aqil ◽  
Farhan J. Ahmad ◽  
Yasmin Sultana ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Wistar Rats ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
In Vitro Characterization ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
The Stability

AbstractThe objective of the present study was to develop and characterize nano-ethanolic liposomes (NEL) for transdermal delivery of ibuprofen (IBU). The NEL for transdermal delivery of IBU were prepared by thin film hydration technique and evaluated for vesicle size, shape, entrapment efficiency, transdermal flux, andin vivoanti-inflammatory activity in Wistar rats. The NEL optimized formulation (NEL-Opt) presented vesicle sizes of 32.85±1.98 nm and entrapment efficiency of 86.40±0.55% with improved transdermal flux. The presence of ethanol and flexibility of NEL could be the reasons for better permeation enhancement of IBU via rat’s skin.In vivoanti-inflammatory study of IBU-loaded NEL-Opt gel showed significant reduction (41.18%) of edema in carrageenan-induced rat paw edema as compared to conventional gel of IBU, where reduction of edema was found to be 12.50%. Our results suggest that developed NEL formulations are efficient systems for transdermal IBU delivery against inflammation. The stability study confirmed that the NEL-Opt gel formulation was considerably stable at refrigerator temperature. Our results concluded that NEL are an efficient carrier for transdermal delivery of IBU.

scholarly journals FORMULATION AND EVALUATION OF AMPHOTERICIN B AND MILTEFOSINE COMBINATION NANOVESICLES

2021 ◽  
pp. 74-78
Author(s):  
MULUGETA F. BEZABEH ◽  
KARL A. WERBOVETZ ◽  
K. V. RAMANA MURTHY
Keyword(s):  
Particle Size ◽  
Amphotericin B ◽  
Therapeutic Option ◽  
Entrapment Efficiency ◽  
Ethanol Injection ◽  
Water Composition ◽  
Stirring Rate ◽  
Drug Entrapment Efficiency

Objective: The aim of the present investigation is to formulate and evaluate amphotericin B-miltefosine combination nanovesicles for application in the treatment of visceral leishmaniasis. Methods: Amphotericin B-miltefosine combination (AmB-MTF) nanovesicles were prepared by ethanol injection method. Formulations of nanovesicles were evaluated at varying conditions of lipids composition, drug-lipid proportion, ethanol-water composition and stirring rate, on drug entrapment efficiency and particle size. Results: The study showed that entrapment efficiency was significantly affected (p<0.01) by the effects of lipids composition, drug-lipid proportion, ethanol-water composition, and stirring rate. Particle size of nanovesicles was significantly affected (p<0.05) by drug-lipid proportion and stirring rate. An optimized formulation of amphotericin B-miltefosine nanovesicles was prepared at optimal factors composition of: phosphatidylcholine-cholesterol-stearic acid 20:4:1, drug-lipid 1:8, AmB-MTF 1:1; ethanol-water 1:4 ratios, and stirring rate 1000 rpm. The AmB-MTF 1:1 nanovesicles formulation showed particle size of 145.6 nm, poly dispersity index 0.19, zeta potential-27.3 mV and drug entrapment efficiency 87%. Conclusion: Evaluation of AmB-MTF 1:1 nanovesicles showed development of a successful formulation with very good compatibility, extended drug release, convenient vesicle size and high drug entrapment efficiency. To conclude, AmB-MTF 1:1 nanovesicles formulation could be a safe and reliable therapeutic option over the conventional combination therapy provided further antileishmanial investigations are investigated in vitro and in vivo.

scholarly journals Cross-linked hyaluronic acid gel inhibits metastasis and growth of gastric and hepatic cancer cells: in vitro and in vivo studies

Oncotarget ◽  
2016 ◽  
Vol 7 (40) ◽  
pp. 65418-65428 ◽  
Author(s):  
Ting Lan ◽  
Ji Pang ◽  
Yan Wu ◽  
Miaolin Zhu ◽  
Xiaoyuan Yao ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Cancer Cells ◽  
In Vivo Studies ◽  
Hepatic Cancer ◽  
Acid Gel ◽  
Hyaluronic Acid Gel

scholarly journals Formulation and Evaluation of Floating Alginate Beads of Diclofenac Sodium

2012 ◽  
Vol 11 (1) ◽  
pp. 29-35 ◽  
Author(s):  
Mohammad Abu Taher Rasel ◽  
Moynul Hasan
Keyword(s):  
Diclofenac Sodium ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
In Vitro Dissolution ◽  
Cross Sectional ◽  
Drug Entrapment Efficiency ◽  
Ft Ir ◽  
Usp Apparatus

The objective of this present investigation is to develop gastroretentive sustained release alginate beads of Diclofenac sodium by the ionotropic gelation method. The floating beads were prepared by dispersing Diclofenac sodium together with CaCO3 (as gas forming agent) into a solution of sodium alginate. The resulting solution was then extruded through a 22 gauge syringe needle into 100 ml cross-linking solution containing calcium chloride (1% w/v) plus acetic acid (10% v/v). Prepared beads were evaluated for their encapsulation efficiency, buoyancy test, FT-IR spectroscopy, scanning electron microscopy (SEM) and release behaviour. In vivo floating behaviour was studied by sonography. The drug entrapment efficiency was increased with the increment of polymer ratio. All of the formulations (F1 to F5) floated immediately or with a very short lag time and remained floating upto 24 hours. Rough and porous surface was observed in case of surface SEM and many large hollow pores or multiple small hollow pockets were observed in case of cross-sectional SEM of beads. In vivo floating behaviour of the beads was confirmed by ultrasonographic examination of a healthy male volunteer after ingestion of capsule containing floating beads. In vitro dissolution studies were performed for eleven hours into 900 ml 0.1N HCl (pH 1.2) using USP Apparatus II (paddle type) maintained at a temperature of 37ºC and stirred at a speed of 50 rpm. The dissolution study revealed that, after eleven hours the percent of drug release for five formulations were 76.7% (F1), 73.5 % (F2), 72.2 % (F3), 70.56% (F4), and 69.1 % (F5) and all of the formulations followed zero order and Higuchi model. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12484 Dhaka Univ. J. Pharm. Sci. 11(1): 29-35, 2012 (June)

Using cross-linked hyaluronic acid gel to prevent postoperative lumbar epidural space adhesion: in vitro and in vivo studies

2019 ◽  
Vol 29 (1) ◽  
pp. 129-140
Author(s):  
Kun Wang ◽  
Xiao long Li ◽  
Jinbo Liu ◽  
Xiaoliang Sun ◽  
Huilin Yang ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Epidural Space ◽  
In Vivo Studies ◽  
Acid Gel ◽  
Hyaluronic Acid Gel

scholarly journals Study of the Effect of Dillenia indica Fruit Mucilage on the Properties of Metformin Hydrochloride Loaded Spray Dried Microspheres

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Hemanta Kumar Sharma ◽  
Lila Kanta Nath
Keyword(s):  
Controlled Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Release Formulation ◽  
Natural Materials ◽  
Drug Entrapment Efficiency ◽  
Dillenia Indica ◽  
Formulation Parameters ◽  
Surface Morphologies

Natural materials are preferred over synthetic counterparts because of their biodegradable and biocompatible nature. The present work was proposed to utilize mucilage from natural source for the development of controlled release formulation of metformin hydrochloride. Natural mucilaginous substance extracted from Dillenia indica L. (DI) fruit was used in fabricating controlled release microspheres. The microspheres were prepared by spray drying method under different formulation parameters. The prepared microspheres were studied for particle size, drug excipient compatibility, particle shape and surface morphologies, drug entrapment efficiency, mucoadhesivity, and in vitro drug release properties. The prepared microspheres exhibited mucoadhesive properties and demonstrated controlled release of metformin hydrochloride. The study reveals that the natural materials can be used for formulation of controlled release microspheres and would provide ample opportunities for further study.

scholarly journals Effects of Vitamin and Amino Acid-Enriched Hyaluronic Acid Gel on the Healing of Oral Mucosa: In Vivo and In Vitro Study

Medicina ◽  
2021 ◽  
Vol 57 (3) ◽  
pp. 285
Author(s):  
Elena Canciani ◽  
Riccardo Sirello ◽  
Gaia Pellegrini ◽  
Dolaji Henin ◽  
Mariachiara Perrotta ◽  
...  
Keyword(s):  
Wound Healing ◽  
Hyaluronic Acid ◽  
Healing Process ◽  
Third Molar ◽  
In Vitro Study ◽  
Vitro Study ◽  
Acid Gel ◽  
Hyaluronic Acid Gel

Background and Objectives: Wound healing is a dynamic process that can be compromised in patients with chronic and metabolic conditions or unhealthy lifestyles. Numerous medical substances designed for topical use, charged with compounds that promote the healing process, have been developed to improve wound healing, especially in compromised subjects. The present study aimed to extend our understanding of the in vivo effects of a hyaluronic acid gel charged with amino acids (HAplus gel, Aminogam gel® Errekappa Euroterapici spa, Milan, Italy) and study the in vitro effects of the same gel charged with additional substances in an attempt to optimize its formulation. Materials and Methods: In a randomized controlled split-mouth clinical and histological trial, HAplus gel was tested on the gingival tissue of the lower third molar post-extraction socket. The gingiva was collected at the time of extraction (T0) and ten days after the extraction (T1) to be histologically analyzed. During the second stage of the study, culture media with HAplus gel and vitamin C and E at different concentrations (TEST) were tested on human gingival fibroblasts and compared to the HAplus-enriched medium (HA-Control). Results: Histological and immunohistochemical analysis of collected gingiva showed higher microvascular density and collagen fibers organized in closely packed and well-oriented bundles in sites treated with HAplus gel. In the in vitro study, all TEST groups showed an increased viability from 24 h to 48 h. After 24 h, the viability percentage in all experimental groups was below 100% of the HA-Control, demonstrating a mild toxicity. After 48 h from seeding, the TEST groups’ viability grew significantly compared to HA-Control. Conclusions: These encouraging preliminary results suggest that the use of HAplus gel enriched with vitamins C and E may be beneficial in patients with conditions that impair soft tissue healing.

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