Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis
Bone-specific functionalization strategies on liposomes are promising approaches to delivering the drug in osteoporotic conditions. This approach delivers the drug to the bone surface specifically, reduces the dose and off-target effects of the drug, and thereby reduces the toxicity of the drug. The...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/2/608 |
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| author | Sagar Salave Suchita Dattatray Shinde Dhwani Rana Bichismita Sahu Hemant Kumar Rikin Patel Derajram Benival Nagavendra Kommineni |
| author_facet | Sagar Salave Suchita Dattatray Shinde Dhwani Rana Bichismita Sahu Hemant Kumar Rikin Patel Derajram Benival Nagavendra Kommineni |
| author_sort | Sagar Salave |
| collection | DOAJ |
| description | Bone-specific functionalization strategies on liposomes are promising approaches to delivering the drug in osteoporotic conditions. This approach delivers the drug to the bone surface specifically, reduces the dose and off-target effects of the drug, and thereby reduces the toxicity of the drug. The purpose of the current research work was to fabricate the bone-specific peptide conjugated pegylated nanoliposomes to deliver anabolic drug and its physicochemical evaluations. For this, a bone-specific peptide (SDSSD) was synthesized, and the synthesized peptide was conjugated with a linker (DSPE-PEG2000-COOH) to obtain a bone-specific conjugate (SDSSD-DSPE). Purified SDSSD-DSPE was characterized by HPLC, Maldi-TOF, NMR, and Scanning Electron Microscope/Energy Dispersive Spectroscopy (SEM/EDS). Further, peptide-conjugated and anabolic drug-encapsulated liposomes (SDSSD-LPs) were developed using the ethanol injection method and optimized by Central Composite Design (CCD) using a statistical approach. Optimized SDSSD-LPs were evaluated for their physicochemical properties, including surface morphology, particle size, zeta potential, in vitro drug release, and bone mineral binding potential. The obtained results from these studies demonstrated that SDSSD-DSPE conjugate and SDSSD-LPs were optimized successfully. The particle size, % EE, and zeta potential of SDSSD-LPs were observed to be 183.07 ± 0.85 nm, 66.72 ± 4.22%, and −25.03 ± 0.21 mV, respectively. SDSSD-LPs demonstrated a sustained drug release profile. Further, the in vitro bone mineral binding assay demonstrated that SDSSD-LPs deliver the drug to the bone surface specifically. These results suggested that SDSSD-LPs could be a potential targeting approach to deliver the anabolic drug in osteoporotic conditions. |
| first_indexed | 2024-03-11T08:16:41Z |
| format | Article |
| id | doaj.art-389eca2f83f14998ac20a4a58c416790 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T08:16:41Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-389eca2f83f14998ac20a4a58c4167902023-11-16T22:42:14ZengMDPI AGPharmaceutics1999-49232023-02-0115260810.3390/pharmaceutics15020608Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in OsteoporosisSagar Salave0Suchita Dattatray Shinde1Dhwani Rana2Bichismita Sahu3Hemant Kumar4Rikin Patel5Derajram Benival6Nagavendra Kommineni7National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad 382355, IndiaNational Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad 382355, IndiaNational Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad 382355, IndiaNational Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad 382355, IndiaNational Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad 382355, IndiaIntas Pharmaceuticals Ltd., Matoda Village, Ahmedabad 382210, IndiaNational Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad 382355, IndiaCenter for Biomedical Research, Population Council, New York, NY 10065, USABone-specific functionalization strategies on liposomes are promising approaches to delivering the drug in osteoporotic conditions. This approach delivers the drug to the bone surface specifically, reduces the dose and off-target effects of the drug, and thereby reduces the toxicity of the drug. The purpose of the current research work was to fabricate the bone-specific peptide conjugated pegylated nanoliposomes to deliver anabolic drug and its physicochemical evaluations. For this, a bone-specific peptide (SDSSD) was synthesized, and the synthesized peptide was conjugated with a linker (DSPE-PEG2000-COOH) to obtain a bone-specific conjugate (SDSSD-DSPE). Purified SDSSD-DSPE was characterized by HPLC, Maldi-TOF, NMR, and Scanning Electron Microscope/Energy Dispersive Spectroscopy (SEM/EDS). Further, peptide-conjugated and anabolic drug-encapsulated liposomes (SDSSD-LPs) were developed using the ethanol injection method and optimized by Central Composite Design (CCD) using a statistical approach. Optimized SDSSD-LPs were evaluated for their physicochemical properties, including surface morphology, particle size, zeta potential, in vitro drug release, and bone mineral binding potential. The obtained results from these studies demonstrated that SDSSD-DSPE conjugate and SDSSD-LPs were optimized successfully. The particle size, % EE, and zeta potential of SDSSD-LPs were observed to be 183.07 ± 0.85 nm, 66.72 ± 4.22%, and −25.03 ± 0.21 mV, respectively. SDSSD-LPs demonstrated a sustained drug release profile. Further, the in vitro bone mineral binding assay demonstrated that SDSSD-LPs deliver the drug to the bone surface specifically. These results suggested that SDSSD-LPs could be a potential targeting approach to deliver the anabolic drug in osteoporotic conditions.https://www.mdpi.com/1999-4923/15/2/608osteoporosisPTH (1-34)anabolic peptideTargetingboneCentral Composite Design |
| spellingShingle | Sagar Salave Suchita Dattatray Shinde Dhwani Rana Bichismita Sahu Hemant Kumar Rikin Patel Derajram Benival Nagavendra Kommineni Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis Pharmaceutics osteoporosis PTH (1-34) anabolic peptide Targeting bone Central Composite Design |
| title | Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis |
| title_full | Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis |
| title_fullStr | Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis |
| title_full_unstemmed | Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis |
| title_short | Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis |
| title_sort | peptide engraftment on pegylated nanoliposomes for bone specific delivery of pth 1 34 in osteoporosis |
| topic | osteoporosis PTH (1-34) anabolic peptide Targeting bone Central Composite Design |
| url | https://www.mdpi.com/1999-4923/15/2/608 |
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