TY - JOUR
T1 - Avance en la administración transdérmica de calcitonina mediante un emulgel nanoestructurado basado en un portador lipídico
AU - Zahrotunisa,
AU - Surini, Silvia
N1 - Funding Information:
The authors gratefully acknowledge the Ministry of Education, Culture, Research, and Technology of Indonesia for financial support through the magister student research grant with contract number NKB-895/UN2.RST/ HKP.05.00.2022.
Publisher Copyright:
© 2023 Journal of Pharmacy & Pharmacognosy Research.
PY - 2023/1
Y1 - 2023/1
N2 - Context: Peptide-protein drugs have a very important role as therapeutic agents for various diseases. However, their therapeutic use has many barriers to delivery, such as large molecular weight, reduced stability during the manufacturing process and storage, and poor absorption when administered orally. One of peptide-protein drugs is calcitonin, a polypeptide of 32 amino acids used to overcome high levels of calcium in the blood, such as hyperparathyroidism. Nevertheless, drug delivery is still challenging to develop. Aims: To evaluate a calcitonin nanostructured lipid carrier-based emulgel, which could penetrate through the stratum corneum, and meet the stability requirements. Methods: Four formulas of calcitonin nanostructured lipid carrier (NLC) were prepared by the double emulsion-evaporation method, then all formulas were characterized in terms of particle size, polydispersity index, zeta potential, entrapment efficiency, and particle morphology. Calcitonin NLCs were then formulated into NLC-based emulgel. Further, in vitro penetration and stability of NLC calcitonin emulgel studies were conducted. Results: The 75:1 ratio of total lipid to the drug (F2) was optimal for calcitonin-loaded NLC with a particle size of 135.6 nm, an index polydispersity of 0.1, the zeta potential of 34.7 mV, and an entrapment efficiency of 99.6%. According to the percutaneous penetration study, the calcitonin NLC-based-emulgel resulted in a fivefold enhancement compared to the non-NLC calcitonin emulgel. Moreover, the stability study illustrated calcitonin levels after six months were 46.09-60.95% and 43.45-68.59% at storage conditions of 5 ± 3ºC and 25 ± 2ºC/RH 60 ±5 %, respectively. Conclusions: The calcitonin NLC-based-emulgel produced a fivefold enhancement permeation through the stratum corneum.
AB - Context: Peptide-protein drugs have a very important role as therapeutic agents for various diseases. However, their therapeutic use has many barriers to delivery, such as large molecular weight, reduced stability during the manufacturing process and storage, and poor absorption when administered orally. One of peptide-protein drugs is calcitonin, a polypeptide of 32 amino acids used to overcome high levels of calcium in the blood, such as hyperparathyroidism. Nevertheless, drug delivery is still challenging to develop. Aims: To evaluate a calcitonin nanostructured lipid carrier-based emulgel, which could penetrate through the stratum corneum, and meet the stability requirements. Methods: Four formulas of calcitonin nanostructured lipid carrier (NLC) were prepared by the double emulsion-evaporation method, then all formulas were characterized in terms of particle size, polydispersity index, zeta potential, entrapment efficiency, and particle morphology. Calcitonin NLCs were then formulated into NLC-based emulgel. Further, in vitro penetration and stability of NLC calcitonin emulgel studies were conducted. Results: The 75:1 ratio of total lipid to the drug (F2) was optimal for calcitonin-loaded NLC with a particle size of 135.6 nm, an index polydispersity of 0.1, the zeta potential of 34.7 mV, and an entrapment efficiency of 99.6%. According to the percutaneous penetration study, the calcitonin NLC-based-emulgel resulted in a fivefold enhancement compared to the non-NLC calcitonin emulgel. Moreover, the stability study illustrated calcitonin levels after six months were 46.09-60.95% and 43.45-68.59% at storage conditions of 5 ± 3ºC and 25 ± 2ºC/RH 60 ±5 %, respectively. Conclusions: The calcitonin NLC-based-emulgel produced a fivefold enhancement permeation through the stratum corneum.
KW - calcitonin
KW - emulgel
KW - nanostructured lipid carrier
KW - peptide-protein drug
KW - transdermal
UR - http://www.scopus.com/inward/record.url?scp=85149922719&partnerID=8YFLogxK
U2 - 10.56499/jppres22.1538_11.1.198
DO - 10.56499/jppres22.1538_11.1.198
M3 - Article
AN - SCOPUS:85149922719
SN - 0719-4250
VL - 11
SP - 198
EP - 207
JO - Journal of Pharmacy and Pharmacognosy Research
JF - Journal of Pharmacy and Pharmacognosy Research
IS - 1
ER -