Effect of Hydrophile-Lipophile Balance (HLB) of Mixed Surfactants on In-Vitro Release Profile of Ibuprofen from Semi-Synthetic Suppository Bases

2021 ◽  
Vol 17 (1) ◽  
pp. 109-117
Author(s):  
A.A. Adeleke ◽  
F.A. Oladimeji
Keyword(s):  
Drug Release ◽  
Physical Properties ◽  
In Vitro Release ◽  
Release Profile ◽  
Release Mechanism ◽  
Mixed Surfactants ◽  
Fusion Method ◽  
Vitro Release ◽  
Release Profiles

Background: The emphasis on the use of surfactants in enhancing drug release from fatty suppository bases has always been on the concentration and type of surfactants. However, the Hydrophile-Lipophile Balance (HLB) of the surfactants added can be of significant effect.Objective: The study aimed at evaluating the effect of HLB of the incorporated mixed surfactants on the physical and release properties of Ibuprofen suppositories formulated with semi-synthetic fatty bases.Methodology: The preparations were carried out using 1 g mould. Ibuprofen suppositories, each containing 200 mg of Ibuprofen with semi-synthetic fatty bases (Witepsol® H15, Suppocire® CM), were prepared by fusion method. Mixed surfactants (Span® 80 and Tween® 80) were added at 4 %w/w in varied ratios to give HLB values of 4.3 to 15.0. The physical properties and release profile of the suppositories were evaluated using established procedures.Results: The physical properties of the suppositories met the standard specified in the BP. Addition of mixed surfactants greatly influenced the release of the Ibuprofen from the formulations with optimum release at lipophilic HLB (4.3) and hydrophilic HLB (12.0) for formulations in Suppocire® CM and Witepsol® H15, respectively. The release parameters majorly fitted into Higuchi’s model. The release mechanism was non-Fickian and Fickian for formulations in Suppocire® CM and Witepsol® H15, respectively.Conclusion: The variations observed in the release profiles of Ibuprofen from the suppository bases indicate that HLB value of mixed surfactants can be employed in modifying drug release from semi-synthetic fatty bases

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

Development of colon targeted matrix tablets of Metformin HCl using various concentration of selected polymers

2017 ◽  
Vol 1 (1) ◽  
pp. 01-02
Author(s):  
Swathi Goli
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Physical Changes ◽  
Metformin Hcl

The aim of the present study was to develop colon targeted matrix tablets of Metformin HCl using various conc. of selected polymers such as HPMC, Ethyl Cellulose Guar gum and combination of the same. Tablets were prepared by direct compression method and both pre-compression and post- compression parameters for all batches shows in the acceptable ranges. Short term accelerated stability studies was performed according to ICH guidelines temperature of 400±20 and relative humidity of 75%±5% RH to study any physical changes and chemical decomposition of drug, no formulation shown any physical or chemical changes. The compatibility of drugs, polymers and excipients were determined by FT-IR Spectroscopy results showed that the drug was compatible with polymers and all excipients. Dissolution studies were performed for 12 hours study in 1.2 pH for first 2 hrs then in 7.4 pH for next 3hrs followed by 6.8pH phosphate buffer at the temperature of 37±0.50C at 100rpm. The dissolution data so obtained was fitted to various mathematical kinetic models and the drug release followed mixed order and Higuchi’s model. To study release mechanism of drug from matrices the data were fitted to Koresmeyer-Peppas model and the release. In –vitro release profile of Metformin HCl from various polymers showed that drug increasing the conc. of polymers resulted in reduction in the release rate of drug (MTF1 to MTF12). Formulation containing combination of E.C-G.G, HPMC-G.G and E.C-HPMC showed drug release profile for MTF-12 about 38.72% after 12 hrs, MTF-11 about 40.66% after 12 hrs, for MTF-10 about 45.45% after 12 hrs. This is an indicative of retardation of drug release when polymer combination was changed. Results showed that the tablets with higher binding concentration showed minimum drug release. Combination of polymers shows greater retarding of drug release.

DEVELOPMENT OF FLOATING GASTRORETENTIVE DRUG DELIVERY SYSTEM BASED ON A NOVEL EXCIPIENT FOR METFORMIN HYDROCHLORIDE USING MIXTURE DESIGN

2020 ◽  
pp. 62-71
Author(s):  
R. PAWAR ◽  
S. JAGDALE ◽  
D. RANDIVE
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Mixture Design ◽  
Release Profile ◽  
Metformin Hydrochloride ◽  
Matrix Tablet ◽  
Vitro Release

Objective: The present study aimed to develop a new SR metformin hydrochloride (MH) gastroretentive formulation with novel excipient (NE), which has better floatation and can be prepared with more simple pharmaceutical techniques for the treatment of diabetes Mellitus. Methods: A gastro-retentive floating matrix tablet (GFT) formulation of MH was prepared using various concentrations of PEO (Polyox WSR-303) and hydroxypropyl methylcellulose K100M (HPMC K100 M) and Floating agent (novel excipient) to achieve desirable TFT, FLT and drug release. The wet granulation method was selected using isopropyl alcohol as a binder for the preparation of tablets. D-optimal non-simplex mixture design was used for the selection of suitable polymer concentrations and floating agents. Release kinetics was used to determine the mechanism of drug release. Results: It was observed that GFT with optimum quantities of PEO, HPMC K100M, and the floating agent showed 100 % of drug release in 24h with FT up to 24h and minimum FLT of less than 2 min. Formulation with an in vitro release profile slower to the marketed sample was prepared. Conclusion: A sustained-release (GFT) of MH tablets using PEO-, HPMC K100M, and an effervescent system was successfully prepared. AGFT formulation with an in vitro release profile slower to the marketed sample that releases MH for 24h may suitable for once-daily dosing can be prepared.

scholarly journals FORMULATION DEVELOPMENT, EVALUATION AND OPTIMIZATION OF MEDICATED LIP ROUGE CONTAINING NIOSOMAL ACYCLOVIR FOR THE MANAGEMENT OF RECURRENT HERPES LABIALIS

2017 ◽  
Vol 9 (6) ◽  
pp. 21 ◽  
Author(s):  
Rajalakshmi S. V. ◽  
Vinaya O. G.
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Herpes Labialis ◽  
Formulation Development ◽  
Recurrent Herpes ◽  
Vitro Release

Objective: Aim of the study was to formulate, evaluate and optimize medicated Lip rouge containing acyclovir encapsulated inside a novel vesicular carrier, niosome so that the formulation can improve its membrane penetration. Formulating as a cosmetic Lip rouge formulation will also improve patient compliance in the treatment of herpes labialis.Methods: Acyclovir niosomes were prepared by thin film hydration method. Niosomes were evaluated and were optimized by considering the entrapment efficiency and in vitro release profile. The optimized niosomes were incorporated into lipstick, lip balm and lip rouge for selecting the best lip formulation. Based on the in vitro release profile, ease of application and properties of prepared formulations lip rouge was selected and further evaluations were carried out.Results: Among the six formulations of niosomes NF2 has showed 88.49 % entrapment efficiency and 86.97% cumulative drug release in 8 h. The formulation was optimized considering both entrapment efficiency and in vitro release. The optimized formulation of niosomes was incorporated into Lipstick, lip balm and lip rouge. The evaluation results of lipstick, lip balm and lip rouge for in vitro release suggested lip rouge as the best formulation. The percentage cumulative release of drug from optimized lip rouge at the end of 8 h was 84.77%. The percentage cumulative drug release in ex vivo studies for 8 h was 60.88 %.Conclusion: The results suggested that prepared lip rouge containing acyclovir niosomes can effectively deliver the drug than the marketed acyclovir cream and successful therapy of Recurrent Herpes labialis can be achieved.

scholarly journals Formulation and Evaluation of Bi-Layer Tablets of Ketorolac Tromethamine

2021 ◽  
Vol 11 (1) ◽  
pp. 36-41
Author(s):  
Dhaval M. Patel ◽  
Riddhi Trivedi ◽  
Hardik Patel
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Immediate Release ◽  
Release Profile ◽  
Hydrophilic Polymers ◽  
Ketorolac Tromethamine ◽  
Vitro Release ◽  
Gastro Retentive

The objective of the present study was to develop and evaluate bi-layer tablets of Ketorolac tromethamine, a nonsteroidal antiinflammatory drug with short half-life, that are characterized by initial burst drug release in the stomach and comply with the release requirements of sustained-release products. Each of the proposed bi-layer tablets is composed of an immediate-release layer and a sustained-release layer, anticipating rapid drug release that starts in the stomach to rapidly alleviate the symptoms and continues in the intestine to maintain protracted analgesic effect. Gastro retentive Bi-Layer tablets of Ketorolac Tromethamine were prepared by using hydrophilic polymers with direct compression on floating – matrix technology and evaluated. Ketorolac tromethamine is freely soluble in water, so it is suitable to develop it as gastro retentive bi-layer tablets using hydrophilic polymers. The developed formulation is equivalent to calculated theoretical drug profile in view of its in vitro release. Immediate release layer was prepared by using dry granulation method in which ac-di sol used as a disintigrant for immediate release of drug. Sustained release layer formulated by using HPMC as release retardant, two grades of HPMC that are HPMC K4M and HPMC K100M used to get sustained release profile for 24 hr. Various trial batches are taken to get desired release profile. Ketorolac tromethamine release from the developed floating formulation followed Higuchi model and nonFickian diffusion is found to be the main mechanism of drug release. The manufacturing procedure was found to be reproducible and formulations were stable after one month of stability studies. Keywords: FTIR; Gastro retentive bilayer; ketorolac tromethamine; in vitro release; stability; higuchi.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

2019 ◽  
Vol 9 (1) ◽  
pp. 76-85 ◽  
Author(s):  
R. Nithya ◽  
K. Siram ◽  
R. Hariprasad ◽  
H. Rahman
Keyword(s):  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Mcf7 Cells ◽  
Solid Lipid ◽  
Cancerous Cells ◽  
Vitro Release

Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations. Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells. Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line. Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

Sign in / Sign up

Export Citation Format

Share Document