scholarly journals Formulation and evaluation of detarium oil based organogel for sustained release of metronidazole via topical delivery

2021 ◽  
Vol 17 (2) ◽  
pp. 96-104
Author(s):  
Margaret O. Ilomuanya ◽  
Uloma N. Ubani-Ukoma ◽  
Abimbola A. Sowemimo ◽  
Gbemisola W. Akande ◽  
Pal Kunal
Keyword(s):  
Sustained Release ◽  
Liquid Paraffin ◽  
Topical Delivery ◽  
Drug Formulation ◽  
Surfactant Mixtures ◽  
Microscopic Studies ◽  
Spherical Structures ◽  
Model Drug ◽  
Conventional Oils

The rationale for this study was to increase the absorption of model drug metronidazole by formulating an organogel using detarium oil in place of conventional oils used in drug formulation such as liquid paraffin. The organogels were prepared by fluid-filled mechanism using metronidazole as the model drug. The drug-surfactant mixtures were dissolved in oil followed by the addition of water which led to the formation of organogels at specific compositions. The formulations were analyzed by microscopy, rheology, in vitro drug release and X-ray diffraction (XRD). Microscopic studies revealed the gels contained clusters of water-filled spherical structures. FTIR study showed compatibility of components of the organogels. DSC result showed all the organogels released heat during formation. The viscosity of the organogels showed an elastic flow followed by a non-elastic phase. The cumulative percentagerelease of metronidazole was found to be between 63% and 85% at the end of 10 h, with OGM 9 having the highest release. XRD result indicated the crystalline nature of the organogels. Metronidazole release from the organogels indicated dissolution, shape, size, and surface area dependent release. The results also showed good compatibility of all the excipients. Sustained release metronidazole organogel was successfully developed using detarium oil. Keywords: Organogel; Detarium oil; Metronidazole; Topical delivery

scholarly journals Formulation and Evaluation of Fusidic Acid Emulgel

2020 ◽  
Vol 10 (3-s) ◽  
pp. 169-175
Author(s):  
Ankita Srivastava ◽  
Sharav Desai ◽  
Hitesh Jain ◽  
D.B. Meshram
Keyword(s):  
Antimicrobial Activity ◽  
Drug Release ◽  
Fusidic Acid ◽  
Liquid Paraffin ◽  
Skin Irritation ◽  
Control Release ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Topical Formulation

Emulgel have emerged as one of the most interesting topical delivery system as it has dual control release system i.e gel and emulsion. Topical applications of drug offers many advantages for delivering drug directly to the site of action and deliver the drug for extended period of time at effected site. The major objective behind this formulation is to enhance topical delivery of hydrophobic drug (Fusidic acid) by formulating Fusidic acid emulgel by using carbopol 934 as gelling agent. In addition light liquid paraffin as oil, span 20 as emulsifier and propylene glycol as co-surfactant were selected for the preparation of emulgel. Fusidic acid is steroidal bacteriostatic agent produced from Fusidium coccineum fungus belongs to class of steroids but has no corticosteroids effect and which is useful for the treatment of number of infections. Fusidic acid binds to protein and ribosomes and inhibits bacterial protein synthesis. The prepared emulgel were evaluated for their physical appearance, pH determination, viscosity, spreadability, in-vitro drug release, antimicrobial activity, skin irritation study and stability. All the prepared emulgel showed acceptable physical properties. The best formulation E9 shows better drug release when compared to all formulation. Keywords: Emulgel, Carbopol 934, Topical formulation, Antimicrobial activity, optimization, Fusidic acid

scholarly journals Sustained release microspheres of ropinirole hydrochloride: Effect of process parameters

2011 ◽  
Vol 61 (4) ◽  
pp. 363-376 ◽  
Author(s):  
Amelia Avachat ◽  
Pralhad Bornare ◽  
Rakesh Dash
Keyword(s):  
Sustained Release ◽  
Process Parameters ◽  
Liquid Paraffin ◽  
Control Release ◽  
Product Yield ◽  
Water Soluble ◽  
Ropinirole Hydrochloride ◽  
Selection Of ◽  
Sustained Release Microspheres

Sustained release microspheres of ropinirole hydrochloride: Effect of process parameters An emulsion solvent evaporation method was employed to prepare microspheres of ropinirole hydrochloride, a highly water soluble drug, by using ethylcellulose and PEG with the help of 32 full factorial design. The microspheres were made by incorporating the drug in a polar organic solvent, which was emulsified using liquid paraffin as an external oil phase. Effects of various process parameters such as viscosity of the external phase, selection of the internal phase, surfactant selection and selection of stirring speed were studied. Microspheres were evaluated for product yield, encapsulation efficiency and particle size. Various drug/ethylcellulose ratios and PEG concentrations were assayed. In vitro dissolution profiles showed that ethylcellulose microspheres were able to control release of the drug for a period of 12 h.

scholarly journals FORMULATION AND IN-VITRO-IN-VIVO EVALUATION OF ALGINATE-CHITOSAN MICROSPHERES OF GLIPIZIDE BY IONIC GELATION METHOD

2017 ◽  
Vol 10 (7) ◽  
pp. 385 ◽  
Author(s):  
Maya Sharma ◽  
Choudhury Pk ◽  
Suresh Kumar Dev
Keyword(s):  
Sustained Release ◽  
Dosage Form ◽  
Oral Dosage ◽  
Ionic Gelation ◽  
In Vivo Evaluation ◽  
Chitosan Microspheres ◽  
Model Drug ◽  
Effective Use

Objective: The present work is aimed to formulate and evaluate alginate-chitosan microspheres of glipizide for the effective use in the treatment of diabetes.Methods: Sustained release microspheres were prepared by gentle mixing of polymers in water phase with drug by agitation. The polymers used for preparation were sodium alginate and chitosan, which was extruded into 5% calcium chloride solution to produce microspheres by ionic gelation method.Results: Single unit dosage form of Glipizide causes gastric irritation. To convert it in to the multiple unit dosage form will release the drug evenly throughout the stomach which suppresses the irritation. The aim of study towards formulation and evaluation of alginate-chitosan microspheres, which can provide sustained release of the model drug. It shows better in-vitro and in-vivo activity than conventional dosage forms. The work also aims to study various parameters affecting the behavior of microspheres in oral dosage form. Conclusion:  Drugs that are simply absorbed from the gastrointestinal tract (GIT) and having a short half life are eliminated rapidly from the blood flow. To avoid this trouble, the oral sustained release (SR) has been developed as these will release the drug slowly in to the GIT and maintain a stable drug concentration in the serum for a longer period of time.

scholarly journals Non-Invasive Topical Drug-Delivery System Using Hyaluronate Nanogels Crosslinked via Click Chemistry

Materials ◽  
2021 ◽  
Vol 14 (6) ◽  
pp. 1504
Author(s):  
Hyunsik Choi ◽  
Mina Kwon ◽  
Hye Eun Choi ◽  
Sei Kwang Hahn ◽  
Ki Su Kim
Keyword(s):  
Drug Delivery ◽  
Click Chemistry ◽  
Topical Delivery ◽  
Topical Drug Delivery ◽  
Safety Issues ◽  
Non Invasive ◽  
Therapeutic Drugs ◽  
Delivery Routes ◽  
Model Drug

Hyaluronate (HA) has been widely investigated for noninvasive topical drug delivery of chemical drugs and biopharmaceuticals. However, previous noninvasive delivery systems have been facilitated mostly by chemical conjugation of drugs with HA, which can cause reduced therapeutic efficacy and safety issues in chemically modified drugs. Here, HA nanogels were synthesized by crosslinking via “click” chemistry for noninvasive topical delivery of a model drug without chemical modification. The model-drug-encapsulating HA nanogels could be uptaken to the skin melanoma cells in vitro by HA-mediated endocytosis. In addition, histological analysis showed that HA nanogels could be topically delivered to the deep skin and tongue tissues through the noninvasive delivery routes. Taken together, HA nanogels could be effectively used for the noninvasive topical delivery of various therapeutic drugs.

scholarly journals Formulation and Evaluation of Biphasic Gastro Floating Tablets of Nateglinide and Atenolol

2020 ◽  
Vol 11 (3) ◽  
pp. 10906-10922
Keyword(s):  
Sustained Release ◽  
Low Cost ◽  
Diffusion Mechanism ◽  
Amorphous State ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Fixed Dose ◽  
Floating Tablets ◽  
Model Drug

The aim was to design, formulate, and evaluate bilayer gastro floating tablets of an antidiabetic agent, nateglinide (immediate-release layer), and antihypertensive agent, atenolol (sustained-release layer). The solubility of model drug nateglinide was enhanced by using cremophor RH 40 and characterized by FTIR, DSC, XRD, SEM, and in vitro dissolution. It was found that selected ingredients were compatible, and crystalline nateglinide transits to an amorphous state. The gastro-bilayer tablets were directly compressed using the optimized nateglinide (solid dispersion equivalent to 60 mg of nateglinide) immediate-release layer (IRL2) containing different percentage of F-Melt type C and crospovidone and atenolol (50 mg) sustained-release layer (SRL6) using different percentage of HPMC K15, sodium bicarbonate, and MCC. Developed tablets were evaluated and found within the acceptance range as per the guidelines. The release of nateglinide and atenolol from an optimized bilayer tablet (BLT3) was 100 % within 60 min and 12 h, respectively. The floating lag time and total floating time were 2 min and 12 h, respectively. The atenolol sustained-release followed the diffusion mechanism. The combination of nateglinide and atenolol was successfully showed a biphasic release pattern. This formulation may strengthen the fixed-dose combination therapy for diabetes and hypertension at a low cost.

Cytoplasmic Granules in Lymphocytes from Rats Dosed with SK&F 14336-D

1971 ◽  
Vol 29 ◽  
pp. 556-557
Author(s):  
T. G. Merrill ◽  
B. J. Payne ◽  
A. J. Tousimis
Keyword(s):  
Lipid Storage ◽  
Pokeweed Mitogen ◽  
Electron Microscopic ◽  
Cytoplasmic Granules ◽  
Storage Diseases ◽  
Tay Sachs Disease ◽  
Large Numbers ◽  
Microscopic Studies ◽  
Neurovisceral Lipidosis

Rats given SK&F 14336-D (9-[3-Dimethylamino propyl]-2-chloroacridane), a tranquilizing drug, developed an increased number of vacuolated lymphocytes as observed by light microscopy. Vacuoles in peripheral blood of rats and humans apparently are rare and are not usually reported in differential counts. Transforming agents such as phytohemagglutinin and pokeweed mitogen induce similar vacuoles in in vitro cultures of lymphocytes. These vacuoles have also been reported in some of the lipid-storage diseases of humans such as amaurotic familial idiocy, familial neurovisceral lipidosis, lipomucopolysaccharidosis and sphingomyelinosis. Electron microscopic studies of Tay-Sachs' disease and of chloroquine treated swine have demonstrated large numbers of “membranous cytoplasmic granules” in the cytoplasm of neurons, in addition to lymphocytes. The present study was undertaken with the purpose of characterizing the membranous inclusions and developing an experimental animal model which may be used for the study of lipid storage diseases.

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

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