Lercanidipine hydrochloride loaded self-nanoemulsifying: A novel approach drug delivery for hypertension treatment as single dose liquid oral ampoule

N.A.

Makale detayları

Lercanidipine hydrochloride loaded self-nanoemulsifying: A novel approach drug delivery for hypertension treatment as single dose liquid oral ampoule

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.29 Issue 2, pp.806-819

Belge Tipi:

Makale

Yayın Tarihi:

8/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001341725

pISSN:

2630-6344

Anahtar kelimeler:

Özet:

 Lercanidipine Hydrochloride LRCH is a third-generation dihydropyridine calcium channel blocker. It is a safe antihypertensive drug with a protective effect on the kidneys in hypertensive patients who have diabetes or chronic renal disease. It is practically insoluble in water and belongs to the Biopharmaceutical Classification System BCS Class II. It has a high lipophilic nature due to its Log P value of 6.42, distinguishing it from older dihydropyridines. Its oral bioavailability is only 10, and erratic absorption is observed due to its extensive first-pass metabolism. However, when taken with food, especially high-fat foods, its bioavailability can increase 30-40. In this study, based on the pharmacokinetic characteristics of LRCH, it is suggested that this drug is an excellent candidate for formulating a unique self-nano emulsifying drug delivery system SNEDDS oral dosage form to overcome the challenges associated with this drug using peppermint oil as an oil phase, Tween 20 as a surfactant, and propylene glycol as a co-surfactant. Pseudo-ternary phase diagrams generated by varying ratios of surfactant and co-surfactant 1:1, 2:1, 3:1, as well as 4:1. The results showed that we successfully loaded LRCH in SNEDDS liquid formulation with different Smix ratios in excellent properties, ranging from 9 - 24 seconds emulsification time, 9.415 - 32.14 nm droplet size, 0.11 - 0.699 PDI, 98.265 - 99.889  drug content, and higher dispersion rate over 97 during 60 min. The Fourier transform infrared spectroscopy FTIR data show that the excipients are compatible with the drug, and the globules are indeed nano-sized and spherical, as confirmed by atomic force microscopy AFM.

 Lercanidipine Hydrochloride LRCH is a third-generation dihydropyridine calcium channel blocker. It is a safe antihypertensive drug with a protective effect on the kidneys in hypertensive patients who have diabetes or chronic renal disease. It is practically insoluble in water and belongs to the Biopharmaceutical Classification System BCS Class II. It has a high lipophilic nature due to its Log P value of 6.42, distinguishing it from older dihydropyridines. Its oral bioavailability is only 10, and erratic absorption is observed due to its extensive first-pass metabolism. However, when taken with food, especially high-fat foods, its bioavailability can increase 30-40. In this study, based on the pharmacokinetic characteristics of LRCH, it is suggested that this drug is an excellent candidate for formulating a unique self-nano emulsifying drug delivery system SNEDDS oral dosage form to overcome the challenges associated with this drug using peppermint oil as an oil phase, Tween 20 as a surfactant, and propylene glycol as a co-surfactant. Pseudo-ternary phase diagrams generated by varying ratios of surfactant and co-surfactant 1:1, 2:1, 3:1, as well as 4:1. The results showed that we successfully loaded LRCH in SNEDDS liquid formulation with different Smix ratios in excellent properties, ranging from 9 - 24 seconds emulsification time, 9.415 - 32.14 nm droplet size, 0.11 - 0.699 PDI, 98.265 - 99.889  drug content, and higher dispersion rate over 97 during 60 min. The Fourier transform infrared spectroscopy FTIR data show that the excipients are compatible with the drug, and the globules are indeed nano-sized and spherical, as confirmed by atomic force microscopy AFM.

 Lercanidipine Hydrochloride LRCH is a third-generation dihydropyridine calcium channel blocker. It is a safe antihypertensive drug with a protective effect on the kidneys in hypertensive patients who have diabetes or chronic renal disease. It is practically insoluble in water and belongs to the Biopharmaceutical Classification System BCS Class II. It has a high lipophilic nature due to its Log P value of 6.42, distinguishing it from older dihydropyridines. Its oral bioavailability is only 10, and erratic absorption is observed due to its extensive first-pass metabolism. However, when taken with food, especially high-fat foods, its bioavailability can increase 30-40. In this study, based on the pharmacokinetic characteristics of LRCH, it is suggested that this drug is an excellent candidate for formulating a unique self-nano emulsifying drug delivery system SNEDDS oral dosage form to overcome the challenges associated with this drug using peppermint oil as an oil phase, Tween 20 as a surfactant, and propylene glycol as a co-surfactant. Pseudo-ternary phase diagrams generated by varying ratios of surfactant and co-surfactant 1:1, 2:1, 3:1, as well as 4:1. The results showed that we successfully loaded LRCH in SNEDDS liquid formulation with different Smix ratios in excellent properties, ranging from 9 - 24 seconds emulsification time, 9.415 - 32.14 nm droplet size, 0.11 - 0.699 PDI, 98.265 - 99.889  drug content, and higher dispersion rate over 97 during 60 min. The Fourier transform infrared spectroscopy FTIR data show that the excipients are compatible with the drug, and the globules are indeed nano-sized and spherical, as confirmed by atomic force microscopy AFM.

 Lercanidipine Hydrochloride LRCH is a third-generation dihydropyridine calcium channel blocker. It is a safe antihypertensive drug with a protective effect on the kidneys in hypertensive patients who have diabetes or chronic renal disease. It is practically insoluble in water and belongs to the Biopharmaceutical Classification System BCS Class II. It has a high lipophilic nature due to its Log P value of 6.42, distinguishing it from older dihydropyridines. Its oral bioavailability is only 10, and erratic absorption is observed due to its extensive first-pass metabolism. However, when taken with food, especially high-fat foods, its bioavailability can increase 30-40. In this study, based on the pharmacokinetic characteristics of LRCH, it is suggested that this drug is an excellent candidate for formulating a unique self-nano emulsifying drug delivery system SNEDDS oral dosage form to overcome the challenges associated with this drug using peppermint oil as an oil phase, Tween 20 as a surfactant, and propylene glycol as a co-surfactant. Pseudo-ternary phase diagrams generated by varying ratios of surfactant and co-surfactant 1:1, 2:1, 3:1, as well as 4:1. The results showed that we successfully loaded LRCH in SNEDDS liquid formulation with different Smix ratios in excellent properties, ranging from 9 - 24 seconds emulsification time, 9.415 - 32.14 nm droplet size, 0.11 - 0.699 PDI, 98.265 - 99.889  drug content, and higher dispersion rate over 97 during 60 min. The Fourier transform infrared spectroscopy FTIR data show that the excipients are compatible with the drug, and the globules are indeed nano-sized and spherical, as confirmed by atomic force microscopy AFM.

Makale detayları

Lercanidipine hydrochloride loaded self-nanoemulsifying: A novel approach drug delivery for hypertension treatment as single dose liquid oral ampoule

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.29 Issue 2, pp.806-819

Belge Tipi:

Makale

Yayın Tarihi:

8/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001341725

pISSN:

2630-6344

Lercanidipine HCL

self-nano emulsifying

Tween20

pseudo ternary phase diagram

oral ampule

Sayı

Makale detayları

Lercanidipine hydrochloride loaded self-nanoemulsifying: A novel approach drug delivery for hypertension treatment as single dose liquid oral ampoule

Yazarlar: N.A.

Yayıncı: Marmara University

Ana Başlıklar: Pharmacology and Pharmaceutical Sciences (Other)

Dergi: Journal of Research in Pharmacy Vol.29 Issue 2, pp.806-819

Belge Tipi: Makale

Yayın Tarihi: 8/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001341725

pISSN: 2630-6344

Lercanidipine HCL

self-nano emulsifying

Tween20

pseudo ternary phase diagram

oral ampule

Sayı

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmacology and Pharmaceutical Sciences (Other)

Dergi:

Journal of Research in Pharmacy Vol.29 Issue 2, pp.806-819

Belge Tipi:

Makale

Yayın Tarihi:

8/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001341725

pISSN:

2630-6344