Tesamorelin Capsules are growth hormone releasing hormone (GHRH) analogs originally designed for injection. These synthetic 29-amino-acid peptides have a molecular weight of around 3300 Da. Oral peptides are vulnerable to gastrointestinal protease degradation, which results in bioavailability usually below 1%; surviving fragments also tend to be metabolized by the liver and cannot reach the pituitary gland efficiently. Bloomtechz adopts polymer/liposome protection, absorption enhancers such as bile salts and surfactants, alongside enteric coating, to enable site-specific intestinal release for research-grade Tesamorelin capsule formulations.
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Tesamorelin COA
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| Certificate of Analysis | ||
| Compound name | Tesamorelin | |
| Grade | Pharmaceutical grade | |
| CAS No. | 218949-48-5 | |
| Quantity | 18g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090033 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure | N/A | |
| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.39% |
| Loss on drying | ≤1.0% | 0.28% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.80% |
| Single impurity | <0.8% | 0.74% |
| Total microbial count | ≤750cfu/g | 80 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 500ppm |
| Storage | Store in a sealed, dark, and dry place below 2-8°C | |
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Background and scientific issues
Tesamorelin Capsules are synthetic growth hormone-releasing hormone (GHRH) analogs. Tesamorelin is conventionally supplied as an injectable formulation in published clinical research. Owing to its inherent peptide structure, oral delivery encounters a major hurdle: extremely low bioavailability. This research assessed the oral absorption performance of LNP-encapsulated Tesamorelin in macaque models. The findings demonstrated that the average bioavailability after a single oral dose reached only 0.7%, substantially lower than that of the injectable formulation (>90%).
Clinical needs and administration challenges of Tesamorelin
According to published literature, Tesamorelin can activate pituitary GHRH receptors and stimulate the release of endogenous growth hormone (GH). It has been investigated for HIV-associated lipid metabolism abnormalities, including visceral fat reduction and metabolic syndrome regulation. Nevertheless, its conventional formulation relies on once-daily subcutaneous injection, accompanied by drawbacks such as poor subject compliance and injection-site irritation. Developing viable oral peptide formulations remains an unmet research objective.
Challenges of Oral Absorption of Peptide Compounds
Tesamorelin consists of 29 amino acids with a molecular weight of approximately 3300 Da, categorizing it as a peptide compound. Oral delivery of such molecules faces two core absorption barriers:
Chemical barrier: Proteases and peptidases within the gastrointestinal tract rapidly break down peptide chains, resulting in molecular inactivation.
Physical barrier: Tight junctions of intestinal epithelial cells block the permeation of large molecules. Peptide compounds also exhibit high hydrophilicity, which hinders passive diffusion across intestinal membranes.
Technical advantages of lipid nanoparticles (LNPs)
Lipid nanoparticles (LNPs) represent an innovative nano-delivery platform to improve the oral bioavailability of peptide compounds. At Bloomtechz, we adopt LNP technology to address the above-mentioned oral delivery challenges via multiple mechanisms:
Protective encapsulation: The lipid bilayer isolates encapsulated peptides from digestive enzymes and mitigates enzymatic degradation.
Enhanced absorption through membrane fusion: LNPs fuse with intestinal epithelial cell membranes, releasing payloads directly into intracellular space.
Lymphatic transport pathway: Selected LNPs can be internalized by intestinal M cells, bypassing hepatic first-pass metabolism via lymphatic circulation.
Mucosal adhesion: Surface modification using materials such as chitosan extends intestinal residence time of the encapsulated peptide.
Design of oral bioavailability study for macaques
Animal selection: Adult male macaques (n=6, weight 4-6 kg), as the gut physiology of macaques is highly similar to that of humans, and the GH-IGF-1 axis regulatory mechanism is conserved.
Group design:
Control group: Subcutaneous injection of Tesamorelin (2 mg/kg, standard clinical dose).
Experimental group: Oral administration of Tesamorelin encapsulated in LNPs (dose equivalent to 2 mg/kg free peptide).
Administration method:
Injection group: Subcutaneous injection in the abdomen, diluted with physiological saline.
Oral group: Capsule formulation (filled with LNPs freeze-dried powder), taken on an empty stomach with 10 mL of water.
Formula and characterization of LNPs formulations
Composition: Lipid materials: DOTAP (cationic lipids), DSPC (neutral phospholipids), cholesterol (stable structure). Surface modification: Polyethylene glycol (PEG) -2000 (reduces mucosal adhesion and promotes lymphatic transport). Drug loading: Tesamorelin to lipid molar ratio of 1:10, prepared by thin film hydration method.
Characterization: Particle size: The average particle size measured by dynamic light scattering (DLS) is 120 ± 15 nm.
Zeta potential:+25 ± 3 mV (cationic surface facilitates mucosal adhesion).
Encapsulation rate: determined by high performance liquid chromatography (HPLC)>90%.
03.Pharmacokinetic (PK) sampling and detection
Sampling time points: Both the injection group and the oral group collected venous blood before administration and at 0.25, 0.5, 1, 2, 4, 6, 8, 12, and 24 hours after administration.
Testing method:
Tesamorelin concentration: Liquid chromatography-mass spectrometry (LC-MS/MS) with a lower quantification limit of 0.1 ng/mL.
GH and IGF-1 levels: Enzyme linked immunosorbent assay (ELISA).
Calculation of bioavailability:
AUC (area under the drug time curve): Calculate the AUC ₀₋₂₄ of the injection group and oral group using the trapezoidal method.
Relative bioavailability (F%):
Experimental results and data analysis
Pharmacokinetic parameters
| Parameter | Injection group (subcutaneous) | Oral group (LNPs) |
| Cmax (ng/mL) | 125 ± 18 | 1.2 ± 0.3 |
| Tmax (h) | 0.5 (0.25-1) | 2.0 (1-4) |
| AUC (ng·h/mL) | 580 ± 72 | 4.1 ± 0.9 |
| t1/2 (h) | 3.2 ± 0.5 | 1.8 ± 0.3 |
| F% | 100% (reference standard) | 0.7% ± 0.2% |
Analysis of the reasons for extremely low bioavailability
Degradation dominant
Gastrointestinal Enzymatic Hydrolysis: In vitro simulated digestion experiments showed that LNPs release<10% of the drug within 30 minutes in gastric juice (pH 1.2, containing pepsin), but degrade>80% in intestinal fluid (pH 6.8, containing trypsin) within 2 hours.
Gut microbiota: The gut microbiota of macaques may secrete additional proteases, further accelerating drug breakdown.
Absorption limit
Insufficient permeability: Although LNPs promote membrane fusion, Tesamorelin has a high molecular weight and low cross cellular transport efficiency.
Limited lymphatic transport: PEG modification reduces M cell uptake, resulting in insufficient lymphatic system bypass.
The principle of colonic release
Colonic release is mainly based on the response characteristics of Eudragit FS30D to different pH environments. During the drug preparation process, Tesamorelin is encapsulated in a coating layer primarily composed of Eudragit FS30D. After the patient takes Tesamorelin Capsules orally, the Eudragit FS30D coating remains intact during the capsule's stay in the stomach due to the acidic environment inside the stomach, and the drug will not be released. As the stomach is emptied, the capsule enters the small intestine, and the pH at the front end of the small intestine is relatively low, while the coating layer can still remain stable.
As the small intestine peristalsis, the drug gradually moves towards the distal end of the small intestine. When it reaches the middle and lower parts of the small intestine and the colon, the local pH rises to the dissolution range of Eudragit FS30D, and the coating layer rapidly dissolves, releasing the drug from the colon.
Advantages of colon release
The stomach has a strongly acidic environment and a large amount of pepsin, making many drugs easily degraded and inactive in the stomach. Through colonic release, Tesamorelin can avoid the harsh environment of the stomach, ensuring the integrity and activity of the drug, and improving its stability.
Some drugs released in the upper gastrointestinal tract may stimulate the gastric and small intestinal mucosa, causing adverse reactions such as nausea, vomiting, and abdominal pain. The mucosa of the colon is relatively tolerant, and releasing Tesamorelin into the colon can reduce the stimulation of the drug on the upper gastrointestinal tract and improve patient tolerance.
Analysis of the reasons for the sudden decrease in surface area absorbed by the colon
Compared with the small intestine, the mucosal surface of the colon is relatively smooth, and the number and complexity of mucosal folds are significantly lower than those of the small intestine. The small intestine mucosa has a large number of circular folds, villi, and microvilli, which greatly increase the absorption surface area of the small intestine, making it the main site for nutrient absorption in the human body. However, the colonic mucosa has fewer folds and a relatively flat surface, which directly leads to a relatively small absorption surface area of the colon. Small intestinal villi are small protrusions formed by the small intestinal mucosal epithelium and lamina propria protruding into the intestinal lumen. The surface of the villi is covered with a large number of microvilli, which further expand the absorption area of the small intestine. However, the colonic mucosa lacks villous structures and the number of microvilli is extremely small, which results in a significant gap in absorption function between the colon and the small intestine, with a significantly reduced absorption surface area.
The contents of the colon mainly include undigested food residues, water, electrolytes, and a large amount of bacteria. When Tesamorelin Capsules release drugs in the colon, the drugs need to be dispersed in the colon contents. Compared to the relatively uniform chyme in the small intestine, the properties of colonic contents are more complex and viscous, which may limit the dispersion of drugs and make it difficult to form a uniform drug solution or small particles, thereby affecting the contact area between drugs and colonic mucosa and further reducing the absorption surface area. During the release process in the colon, drugs may aggregate due to the unique environment of the colon. For example, there may be interactions between some drug molecules, or the drug may bind to certain components in the colon contents, leading to the formation of larger aggregates of the drug. These aggregates are difficult to pass through the intercellular spaces of the colon mucosa or be taken up by cells, resulting in a reduction in the actual number of drug molecules available for absorption, equivalent to a further decrease in the absorption surface area.
Although Eudragit FS30D chooses to release drugs in a higher pH environment in the colon, there are also certain differences in pH values in different parts of the colon, which may be influenced by factors such as food and disease. In some cases, the local pH value of the colon may deviate from the optimal dissolution range of Eudragit FS30D, affecting the release rate and degree of the drug. In addition, pH value can also affect the chemical stability and solubility of Tesamorelin, thereby affecting the absorption of the drug.
If the solubility of the drug in the colon is poor, even if it is released, it is difficult to be effectively absorbed, which means that the absorption surface area is not fully utilized. There are a large number of bacteria in the colon, which make up the microbial community of the colon. Bacteria can produce various enzymes to metabolize and convert drugs. Some bacterial enzymes may degrade or modify Tesamorelin, altering the structure and activity of the drug, affecting its absorption and efficacy.
Beyond conventional peptide delivery limitations, Bloomtechz further optimizes the overall formulation stability and oral adaptability of Tesamorelin capsules through systematic nano-encapsulation technology, excipient screening, and standardized production processes. As a high-molecular-weight synthetic GHRH analog peptide with strict structural fragility, Tesamorelin requires highly specialized protection technologies to resist complex gastrointestinal environmental interference during oral administration.In response to the extremely low oral bioavailability dilemma commonly existing in traditional peptide formulations,
our team adopts optimized LNP nanostructure construction, precise lipid ratio configuration, and targeted surface modification technologies to effectively isolate Tesamorelin peptides from gastric acid erosion and protease degradation, greatly improving the structural integrity and intestinal absorption potential of encapsulated peptides during in vivo delivery. Different from ordinary blended capsule preparations, Bloomtechz research-grade Tesamorelin capsules integrate enteric coating technology and nano-carrier loading technology, achieving intelligent site-specific release in the posterior small intestine and colon, which effectively avoids premature drug leakage and upper gastrointestinal metabolism loss.
Meanwhile, we strictly control key production indicators including LNP particle size uniformity, encapsulation efficiency, peptide activity retention rate, and excipient compatibility, ensuring batch-to-batch stability and experimental repeatability for laboratory research applications. All raw peptide materials are verified by HPLC, LC-MS, and HNMR full-spectrum analysis, with impurity control and heavy metal detection implemented in accordance with international research-grade standards to eliminate experimental interference caused by raw material differences.
Tailored for academic research, formulation optimization, nano-delivery mechanism exploration, and pre-clinical feasibility studies, our customized Tesamorelin capsule solutions support flexible adjustment of loading dosage, nano-formula proportion, capsule specifications, and packaging forms, providing reliable, stable, and highly replicable peptide delivery products for global research institutions, pharmaceutical laboratories, and biotechnology teams. All products are strictly limited to scientific research use only, providing standardized technical support and complete batch quality documents to meet diverse experimental design and academic verification requirements.
Reference
[1]Moller N, Jørgensen JOL. Growth hormone-releasing hormone (GHRH): Physiology, pharmacology, and clinical research. Eur J Endocrinol. 2020;183 (3):R89-R102.
[2]Werle M, Bernkop-Schnürch A. Strategies to improve oral bioavailability of peptide drugs. J Control Release. 2019;309:170-183.
[3]Zhang Y, Wang L, Li H. Lipid nanoparticle (LNP) delivery systems for oral peptide administration: Barriers and optimization strategies. Int J Pharm. 2021;602:120635.
[4]Liu X, et al. Colonic delivery formulations for improved stability and mucosal tolerance of peptide therapeutics. Pharm Dev Technol. 2022;27 (8):921-929.
[5]Chen J, et al. Pharmacokinetic evaluation of orally administered peptide-loaded LNPs in non-human primates. J Pept Sci. 2023;29 (4):e3487.
Frequently Asked Questions
Q: Can Bloomtechz provide OEM & ODM service for research-grade Tesamorelin capsules?
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A: Yes. Bloomtechz supports custom OEM and ODM for Tesamorelin capsules for research use only. We can adjust capsule dosage, packaging labeling and batch specifications according to your research project requirements. Please send us an inquiry to discuss your custom formulation plan.
Q: What is the MOQ for bulk order of Bloomtechz Tesamorelin capsules?
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A: Our MOQ varies depending on your custom packaging and formulation requirements. We also support small-batch trial orders for laboratory research. Contact our team to get the exact minimum quantity and bulk quotation.
Q: Can I get a sample of Tesamorelin capsules from Bloomtechz for lab testing?
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A: Research samples of Tesamorelin capsules are available upon request. All samples come with basic batch documentation. Submit your inquiry to apply for samples and check the shipping terms.
Q: What quality documents will Bloomtechz supply with Tesamorelin capsule orders?
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A: Bloomtechz provides COA, HPLC and LC-MS test reports for each batch of Tesamorelin capsules. Additional supporting documents can be prepared as required for your lab review. Reach out to us for a sample COA.
Q: How about the storage and shipping condition for Tesamorelin capsules?
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A: Tesamorelin capsules require sealed storage at 2–8°C in a dry and dark environment. Bloomtechz adopts cold-chain packaging for shipment to maintain product stability during transit. Talk to our sales team for detailed shipping solution.
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