Design and development of solid nanoparticulate dosage forms of telmisartan for bioavailability enhancement by integration of experimental design and principal component analysis

Patel, Jay; Dhingani, Anjali; Garala, Kevin; Raval, Mihir; Sheth, Navin

doi:10.1016/j.powtec.2014.03.001

Cited by 33 publications

(15 citation statements)

References 58 publications

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“…Therefore, it is necessary to improve the solubility and dissolution rate of TMS. Several studies have been conducted to improve the solubility and dissolution of TMS including co-grinding TMS with polyvinyl alcohol 3 , formation of solid nanoparticles 4 , inclusion complex of TMS and b-cyclodextrins 5 , formation of cocrystalline phase with several coformers 6,7 , formation amorphous solid dsipersion 8 .…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Zaini¹,

Fitriani²,

Effendy³

et al. 2017

Orient. J. Chem

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Telmisartan (TMS), an antihypertensive drug, is classified as class II according to Biopharmaceutical Classification System (BCS) with low solubility and high permeability. The purpose of this study was to prepare and characterize solid dispersion of TMS with hidroxypropyl methyl cellulose (HPMC) E5 LV to increase the solubility. Solid dispersion was prepared in three different ratio TMS:HPMC 2:1, 1:1, and 1:2 (w/w) by co-grinding method for 60 minutes. Solubility test was conducted in distilled water for 72 hours and the amount of TMS was determined by spectrophotometry UV. Result of Powder X-Ray Diffraction (PXRD) showed a decrease in intensity of TMS in accordance with the amount of HPMC E5 LV in solid dispersion. Fourier Transform Infra-Red(FT-IR)Spectra showed no significant shift of wavelength. Scanning Electron Microscopy (SEM) result presented the crystalline form of TMS, while both physical mixture and solid dispersion at different ratio showed TMS stick on the surface of HPMC E5 LV. Thermogram of Differential Scanning Calorimetry (DSC) showed an incline of endotherm peak as the ratio HPMC E5 LV increased. The solubility result of intact TMS was 0.49±0.03µg/mL, while the physical mixture and solid dispersion 2:1, 1;1 and 1:2 were 1.87±0.18 µg/mL, 5.36±0.48 µg/mL, 7.24±1.73µg/mL, and 14.89±1.49 µg/mL, respectively. In conclusion, solid dispersion of telmisartan-HPMC E5 LV enhanced the solubility of TMS.

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Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Zaini¹,

Fitriani²,

Effendy³

et al. 2017

Orient. J. Chem

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“…Patel et al. (2014), have optimized the telmisartan particle size using the milling (drug, stabilizer, and water) and lyophilization techniques and achieved the particle size of 334.67 nm.…”

Section: Resultsmentioning

confidence: 99%

“…Telmisartan is readily ionizable, and hence its solubility is pH dependent . However, due to its high lipophilicity, low aqueous solubility (9.9 µg mL −1 ), and low oral bioavailability (40%), the oral administration has resulted in poor absorption …”

Section: Introductionmentioning

confidence: 99%

“…One of the main focuses of pharmaceutical technology is to develop a novel strategy to enhance the solubility and bioavailability of poorly water‐soluble drugs without altering the molecular structure. According to BCS the bioavailability of a poorly water‐soluble drug can be improved by increasing the solubility and dissolution rate in aqueous gastrointestinal fluids . One method of improving the solubility and dissolution rate of the drug is to reduce the particle size so that there is an increase in the interfacial surface area.…”

Section: Introductionmentioning

confidence: 99%

“…This can be achieved by impeded crystallization to form amorphous particles . Various methods including solid dispersion, nanosuspension, complexation with hydroxypropyl β cyclodextrin, co‐crystals, and self micro‐emulsifying, formulation have been employed to enhance the dissolution rate of various poorly water‐soluble drugs including telmisartan. Telmisartan has a weak base (pKa 3.6) and it is soluble in hydrochloric acid solution.…”

Section: Introductionmentioning

confidence: 99%

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Ultrasound‐Assisted Anti‐Solvent Crystallization of Telmisartan Using Dimethyl Sulfoxide as Organic Solvent

Sharma

Desai

Patel

2018

Crystal Research and Technology

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In recent years, ultrasound assisted anti‐solvent crystallization has emerged as an excellent approach to reduce the particle size of poorly water‐soluble drugs, thereby achieving improvement in the solubility and bioavailability. In the present study, this concept is employed for telmisartan by studying various critical parameters like the effect of sonication time, sonication amplitude, drug solution concentration, solvent to anti‐solvent ratio, injection rate and crystallization temperature. The particle size of the commercial telmisartan is reduced from 10 µm to 200 nm by anti‐solvent crystallization method by applying 60% ultrasound amplitude for 15 min with 10 mg mL−1 drug concentration, 1:3 of solvent to anti‐solvent ratio, and 10 mL min−1 of injection rate at 30 °C. Physicochemical characteristics; morphology, crystalline structure, the presence of other chemical compounds, enthalpy change, and the melting point of a recovered drug are analyzed using various analytical tools. It is possible to achieve nanoparticles of telmisartan by symbiotic effect of sonication with anti‐solvent crystallization.

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Nanotechnology‐Based Strategies for Extended‐Release Delivery of Angiotensin Receptor Blockers (ARBs): A Comprehensive Review

Haji Ali,

Shirvaliloo,

Fathi‐Karkan

et al. 2023

Chemistry & Biodiversity

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There has been a significant shift in the perception of hypertension as an important contributor to the global disease burden. Approximately 6% and 8% of pregnancies are affected by hypertension, which can adversely affect the mother and the fetus. Furthermore, a hypertensive individual is at increased risk of developing kidney disease, arterial hardening, eye damage, and strokes. Using angiotensin receptor blockers (ARBs) is widespread in treating hypertension, heart failure, coronary artery disease, and diabetic nephropathy. Despite this, some ARBs have limited use due to their poor oral bioavailability and water solubility. To tackle this, a variety of nanoparticle (NP)‐based systems, such as polymeric NPs (i.e., dendrimers), polymeric micelles, polymer‐drug conjugates, lipid NPs, nanoemulsions, self‐emulsifying drug delivery systems (SEDDS), solid lipid NPs (SLNs), nanostructured lipid carriers (NLCs), carbon‐based nanocarriers, inorganic NPs, and nanocrystals, have been recently developed for efficient delivery of losartan, Valsartan (Val), Olmesartan (OLM), Telmisartan (TEL), Candesartan, Eprosartan, Irbesartan, and Azilsartan to target cells. This review article provides a literature‐based comparison of the various classes of ARBs, their mechanisms of action, and an overview of the nanoformulations developed for ARB delivery and successfully applied to managing hypertension, diabetic complications, and other conditions.

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Design and development of solid nanoparticulate dosage forms of telmisartan for bioavailability enhancement by integration of experimental design and principal component analysis

Cited by 33 publications

References 58 publications

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Ultrasound‐Assisted Anti‐Solvent Crystallization of Telmisartan Using Dimethyl Sulfoxide as Organic Solvent

Nanotechnology‐Based Strategies for Extended‐Release Delivery of Angiotensin Receptor Blockers (ARBs): A Comprehensive Review

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