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Fulltext Development and evaluation of solid lipid nanoparticles of mometasone furoate for topical delivery

Madan JR, Khude PA, Dua K

Int J Pharm Investig, 2014 Apr;4(2):60-4.
PMID: 25006550 DOI: 10.4103/2230-973X.133047

Solid lipid nanoparticles (SLNs) are the new generation of submicron sized lipid emulsions where liquid lipid (oil) has been substituted by solid lipid. Lipids used in the formulation are safe, stable and biodegradable in nature. SLNs offer various advantages for topical drug delivery like ability of deposition into skin with the reduced systemic exposure and reduced local side-effects along with providing sustained release of drug. Mometasone furoate (MF) is a topical glucocorticoid having anti-inflammatory, anti-pruritic, anti-hyper proliferative activity. Owing to these properties it is recommended in chronic inflammation and psoriasis. In market, MF cream and lotion (0.1%) are available, which show slight skin irritation, burning and common side-effects due to steroids.
Fulltext Polyethylene glycolated PAMAM dendrimers-Efavirenz conjugates

Pyreddy S, Kumar PD, Kumar PV

Int J Pharm Investig, 2014 Jan;4(1):15-8.
PMID: 24678457 DOI: 10.4103/2230-973X.127735

The preparation of novel PEGylated PAMAM (poly-amidoamine) dendrimers for delivery of anti-HIV drug Efavirenz is reported.
Fulltext In vitro and in vivo assessment of piroxicam incorporated Aloe vera transgel

Velam V, Yalavarthi PR, Sundaresan C, Vandana K, Dudala TB, Kodavatikanti H, et al.

Int J Pharm Investig, 2013 Oct;3(4):212-6.
PMID: 24350041 DOI: 10.4103/2230-973X.121303

The aim of the study was to develop piroxicam-Aloe vera gel (PAG) formulation and make a pharmacodynamic evaluation of the formulation.
Fulltext Formulation, characterization, in vitro, in vivo, and histopathological evaluation of transdermal drug delivery containing norfloxacin and Curcuma longa

Dua K, Chakravarthi S, Kumar D, Sheshala R, Gupta G

Int J Pharm Investig, 2013 Oct;3(4):183-7.
PMID: 24350037 DOI: 10.4103/2230-973X.121287

In an attempt for better treatment of bacterial infections and burn wounds, semisolid formulations containing norfloxacin (NF) and natural wound healing agent Curcuma longa were prepared. The rationale behind employing combination of NF and Curcuma longa is to obtain synergistic wound healing effect. The prepared formulations were compared with silver sulfadiazine cream 1%, USP.
Fulltext Performance of transdermal therapeutic systems: Effects of biological factors

Singh I, Morris AP

Int J Pharm Investig, 2011 Jan;1(1):4-9.
PMID: 23071913 DOI: 10.4103/2230-973X.76721

Transdermal drug delivery (TDD) is a technique that is used to deliver a drug into the systemic circulation across the skin. This mechanism of drug delivery route has many advantages, including steady drug plasma concentrations, improved patient compliance, elimination of hepatic first pass, and degradation in the gastrointestinal tract. Over the last 30 years, many transdermal products have been launched in the market. Despite the inherent advantages of TDD and the growing list of transdermal products, one of the major drawbacks to TDD is the occurrence of inter- and intraindividual variation in the absorption of the drug across the skin. A majority of these variations are caused by biological factors, such as gender, age, ethnicity, and skin hydration and metabolism. These factors affect the integrity and the barrier qualities of the skin, which subsequently result in the variation in the amount of drug absorbed. The main objective of this review article is to provide a concise commentary on the biological factors that contribute to the variation in transdermal permeation of drugs across human skin and the available transdermal therapeutic systems that may reduce the variations caused by biological factors.
Fulltext Formulation and evaluation of voriconazole ophthalmic solid lipid nanoparticles in situ gel

Pandurangan DK, Bodagala P, Palanirajan VK, Govindaraj S

Int J Pharm Investig, 2016 Jan-Mar;6(1):56-62.
PMID: 27014620 DOI: 10.4103/2230-973X.176488

In the present investigation, solid lipid nanoparticles (SLNs)-loaded in situ gel with voriconazole drug was formulated. Further, the formulation was characterized for pH, gelling capacity, entrapment efficiency, in vitro drug release, drug content, and viscosity. Voriconazole is an antifungal drug used to treat various infections caused by yeast or other types of fungi. Film hydration technique was used to prepared SLNs from lecithin and cholesterol. Based on the entrapment efficiency 67.2-97.3% and drug release, the optimized formulation NF1 of SLNs was incorporated into in situ gels. The in situ gels were prepared using viscosity-enhancing polymers such as Carbopol and (hydroxypropyl)methyl cellulose (HPMC). Formulated SLN in situ gel formulations were characterized, which showed pH 4.9-7.1, drug content 65.69-96.3%, and viscosity (100 rpm) 120-620 cps. From the characterizations given above, F6 was optimized and evaluated for microbial assay and ocular irritation studies. Microbial assay was conducted by the cup-plate method using Candida albicans as the test organism. An ocular irritation study was conducted on albino rabbits. The results revealed that there was no ocular damage to the cornea, conjunctiva, or iris. Stability studies were carried out on the F6 formulation for 3 months, which showed that the formulation had good stability. These results indicate that the studied SLNs-loaded in situ gel is a promising vehicle for ocular delivery.
Fulltext Solubility enhancement studies on lurasidone hydrochloride using mixed hydrotropy

Madan JR, Pawar KT, Dua K

Int J Pharm Investig, 2015 Apr-Jun;5(2):114-20.
PMID: 25838997 DOI: 10.4103/2230-973X.153390

Low aqueous solubility is a major problem faced during formulation development of new drug molecules. Lurasidone HCl (LRD) is an antipsychotic agent specially used in the treatments of schizophrenia and is a good example of the problems associated with low aqueous solubility. Lurasidone is practically insoluble in water, has poor bioavailability and slow onset of action and therefore cannot be given in emergency clinical situations like schizophrenia. Hence, purpose of this research was to provide a fast dissolving oral dosage form of Lurasidone. This dosage form can provide quick onset of action by using the concept of mixed hydrotropy. Initially, solubility of LRD was determined individually in nicotinamide, sodium citrate, urea and sodium benzoate at concentration of 10, 20, 30 and 40% w/v solutions using purified water as a solvent. Highest solubility was obtained in 40% sodium benzoate solution. In order to decrease the individual hydrotrope concentration mixed hydrotropic agents were used. Highest solubility was obtained in 15:20:5 ratio of Nicotinamide + sodium benzoate + sodium citrate. This optimized combination was utilized in the preparation of solid dispersions by using distilled water as a solvent. Solid dispersions were evaluated for X-ray diffraction, differential scanning calorimetry and Fourier-transform infrared to show no drug-hydrotropes interaction has occurred. This solid dispersion was compressed to form fast dissolving tablets. Dissolution studies of prepared tablets were done using USP Type II apparatus. The batch L3 tablets show 88% cumulative drug release within 14 min and in vitro dispersion time was 32 min. It was concluded that the concept of mixed hydrotropic solid dispersion is novel, safe and cost-effective technique for enhancing the bioavailability of poorly water-soluble drugs. The miraculous enhancement in solubility and bioavailability of Lurasidone is clear indication of the potential of mixed hydrotropy to be used in future for other poorly water-soluble drugs in which low bioavailability is a major concern.
Mechanistic insights into acyclovir-polyethylene glycol 20000 binary dispersions

Venkateskumar K, Parasuraman S, Gunasunderi R, Sureshkumar K, Nayak MM, Shah SA, et al.

Int J Pharm Investig, 2016 Oct-Dec;6(4):194-200.
PMID: 28123988 DOI: 10.4103/2230-973X.195925

The objective of this study is to provide a mechanistic insight into solubility enhancement and dissolution of acyclovir (ACY) by polyethylene glycol20000 (PEG20000).
Fulltext Smartphone usage and increased risk of mobile phone addiction: A concurrent study

Parasuraman S, Sam AT, Yee SWK, Chuon BLC, Ren LY

Int J Pharm Investig, 2017 Jul-Sep;7(3):125-131.
PMID: 29184824 DOI: 10.4103/jphi.JPHI_56_17

Objective: This study aimed to study the mobile phone addiction behavior and awareness on electromagnetic radiation (EMR) among a sample of Malaysian population.

Methods: This online study was conducted between December 2015 and 2016. The study instrument comprised eight segments, namely, informed consent form, demographic details, habituation, mobile phone fact and EMR details, mobile phone awareness education, psychomotor (anxious behavior) analysis, and health issues. Frequency of the data was calculated and summarized in the results.

Results: Totally, 409 respondents participated in the study. The mean age of the study participants was 22.88 (standard error = 0.24) years. Most of the study participants developed dependency with smartphone usage and had awareness (level 6) on EMR. No significant changes were found on mobile phone addiction behavior between the participants having accommodation on home and hostel.

Conclusion: The study participants were aware about mobile phone/radiation hazards and many of them were extremely dependent on smartphones. One-fourth of the study population were found having feeling of wrist and hand pain because of smartphone use which may lead to further physiological and physiological complication.
Fulltext Development of a binary carrier system consisting polyethylene glycol 4000 - ethyl cellulose for ibuprofen solid dispersion

Alagdar GSA, Oo MK, Sengupta P, Mandal UK, Jaffri JM, Chatterjee B

Int J Pharm Investig, 2017 12 1;7(3):142-148.
PMID: 29184827 DOI: 10.4103/jphi.JPHI_54_17

Background and Objective: One of the established strategies to improve solubility and dissolution rate of poorly water-soluble drugs is solid dispersion (SD). Polyethylene glycol (PEG) is used as common carrier despite its stability problem which may be overcome by the addition of hydrophobic polymer. The present research aimed to develop an SD formulation with ibuprofen, a poor water-soluble BCS Class II drug as active pharmaceutical ingredient (API) and PEG 4000-ethyl cellulose (EC) as binary carrier.
Methods: Melt mixing SD method was employed using a ratio of API: binary carrier (1:3.5 w/w) (SDPE). Another SD was prepared using only PEG (SDP) as a carrier for comparative study. The developed formulation was evaluated using optical microscopy, scanning electron microscopy (SEM), determination of moisture content, differential scanning calorimetry (DSC), in vitro dissolution test, attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) and flow properties.
Results: SEM and DSC indicated the conversion of crystalline ibuprofen to fine partly amorphous solid dispersion, which was responsible for the increase in dissolution rate of SD than a physical mixture. The release characteristics within 1 h from the higher to the lower value were the SDPE> SDP> physical mixture. Flow property evaluation using the angle of repose showed no difference between SD and PM. However, by Carr index and Hausner ratio, the flow properties of SDPE was excellent.
Conclusion: The SD formulation with the PEG 4000-EC carrier can be effective to enhance in vitro dissolution of ibuprofen immediate release dosage form.
Fulltext Preparation and characterization of cefuroxime axetil solid dispersions using hydrophilic carriers

Gorajana A, Rajendran A, Yew LM, Dua K

Int J Pharm Investig, 2015;5(3):171-8.
PMID: 26258059 DOI: 10.4103/2230-973X.160857

AIM: The objective of the current study is to increase the dissolution rate of cefuroxime axetil (CA) by formation of binary CA solid dispersion using water soluble carriers such as polyvinylpyrrolidone (PVP K30) and polyethylene glycol (PEG 4000).
METHODS: Solid dispersions (SDs) between CA and PVP K30/PEG 4000 were formed by dissolving both compounds in a common solvent, methanol, which were rotary evaporated at 40°C for 12 h. Physical mixtures between CA and PVP K30/PEG 4000 were also formulated as to compare the efficiency of SDs. The physicochemical properties of CA and all its formulations were then characterized using differential scanning calorimetric analysis (DSC), powder X-ray diffraction studies (PXRD), and Fourier transform infrared spectroscopy (FTIR).
RESULTS: All SD formulations were found to have a higher dissolution rate comparatively to pure CA, while only physical mixtures of PVP K30 were found having a significantly higher dissolution rate. The enhancement of dissolution rate SD by PVP K30 may be caused by increase wettability, solubility, reduction in particle size or the formation of CA β crystalline. Increment of dissolution rate of CA SDs by PEG 4000 similarly may be caused by increase wettability, solubility, and reduction in particle size. This phenomenon may also be caused by amorphization as suggested by DSC and PXRD.
CONCLUSIONS: The SD of CA with PVP K30 and PEG 4000, lends an ample credence for better therapeutic efficacy.