Preparation of Nasal drop

Aim- to prepare and submit the nasal drop.

BACKGROUND

Nasal drop solutions are aqueous liquids that are intended to be sprayed or dropped into the nasal cavities. A large surface area for drug absorption is provided by the microvilli present along the pseudo-stratified columnar epithelial cells of the nasal mucosa in the adult nasal cavity, which has a capacity of about 20 mL.

The nasal tissue is highly vascularized, due to which systemic absorption could be possible in an effective way. Bypassing the liver’s first-pass metabolism is another benefit of nasal delivery. Intranasal bioavailability has been shown to be as effective as injections for some peptides and small-molecule substances.

However, as a compound’s molecular weight rises, bioavailability declines. Proteins made of a greater number of amino acids have low bioavailability. Interestingly some literature suggests that surfactants can enhance the nasal bioavailability of large molecules.¹ In order to maintain normal ciliary function, nasal drops are prepared with similar properties like nasal secretions, therefore the tonicity, pH, and viscosity of the formulation is considered here.

Nasal drops are isotonic and the pH is maintained in the range of 4.5-6.5 with the help of buffers.^1,2 Nasal drops are one of the most simple and convenient drug delivery system. Nasal drops are more conveniently spread than the nasal sprays. However, the lack of dose precision is drawback of this system.³ It has been reported that nasal drops deposit human serum albumin in the nostrils more efficiently than nasal sprays.

Many drugs for systemic and local action are used by nasal route, mainly for local sympathomimetic action for the reduction of nasal congestion, such as ephedrine and naphazoline. Other than these drugs, antibiotics such as rifampicin also used for the treatment of infections.^1,4

More interestingly, nasal drops could be used for the vaccine delivery through nasal route.⁵ Furthermore, along with these active drugs substances, other excipients can also be used for the enhancement of the viscosity or to increase the solubility of the drug substance in the vehicle. Hydroxypropyl methylcellulose is one example of viscosity enhancer commonly used in the nasal solutions. Polysorbate 80 (tween 80) can be used as the solubilizer/ stabilizer in the formulation.⁴

REQUIREMENTS

Apparatus:

Beaker, Stirrer/glass rod, Measuring cylinder, spatula, balance, and storage bottle.

Chemicals:

Rifampin, Hydroxypropyl methylcellulose, Polysorbate, Ascorbic acid, Sodium sulfite and deionized water.

Formulation Table:

Sr.No	Ingredients	Quantity	Role
1	Rifampin	500 mg	Antibiotic
2	Hydroxypropyl methylcellulose	625 mg	Viscosity enhancer
3	Polysorbate 80	150 mg	Solubilizer/stabilizer
4	Ascorbic acid	50 mg	–
5	Sodium sulfite	200 mg	Antioxidant/antimicrobial preservative
3	Purified Water	50 gm	vehicle

PROCEDURE

For the preparation of ear drops, calculate the required quantity of ingredients and weigh it according to the calculated quantity and add it to the beaker, now heat 40 ml of purified water up to 70^oC and add it to the HPMC with stirring. After this, allow the mixture to cool at room temperature, followed by adding the remaining ingredients to it with constant stirring so it will be uniformly distributed. Add the sufficient amount of the purified water to it, for making final volume of the nasal drop.⁴

Use– the rifampin nasal drop is can be used to treat the susceptible infections in nasal cavity.

Label– keep the formulation in clean and dry place, and keep the formulation out of reach of children.

CONCLUSION

Rifampin nasal drop is prepared and submitted. The prepared formulation is mucoadhesive in nature, so it will adhere / retent the active drug substance at the site or area after the administration and show enhanced action.

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REFERENCES

1. Felton L, Remington: Essential of Pharmaceutics, am, J.Pharm.Educ. 2013
2. Pradhan, V., et al., Formulation and evaluation of almotriptan malate nasal drops. Indian Journal of Pharmaceutical Sciences, 2009. 71(6): p. 727.
3. Hemal Tandel, Kiruba Florence, Ambikanandan Misra,9 – Protein and Peptide Delivery through Respiratory Pathway,Editor(s): Ambikanandan Misra,Challenges in Delivery of Therapeutic Genomics and Proteomics, Elsevier, 2011, Pages 429-479, ISBN 9780123849649, https://doi.org/10.1016/B978-0-12-384964-9.00009-8.
4. https://www.uspharmacist.cx`om/article/rifampin-1-nasaldrops
5. Ramvikas, M. Arumugam, S.R. Chakrabarti, K.S. Jaganathan, Chapter Fifteen – Nasal Vaccine Delivery, Editor(s): Mariusz Skwarczynski, Istvan Toth, In Micro and Nano Technologies, Micro and Nanotechnology in Vaccine Development, William Andrew Publishing, 2017, Pages 279-301, ISBN 9780323399814, https://doi.org/10.1016/B978-0-323-39981-4.00015-4.

FAQs

1. Which excipients are commonly used in the nasal drop preparation and mention their roles?

ANS: Hydroxypropyl methyl cellulose (HPMC) and polysorbate 80 (tween 80) are commonly used excipients in the nasal drop preparation, and the HPMC is the viscosity enhancer which increase the viscosity of formulation and polysorbate 80 is used as the solubilizer, which increases the solubility of the active drug substance.

2. What type of water is required in nasal drops?

ANS: The preferred water for use in nasal drop preparation is sterile or distilled water.

3. How to use nasal drops?

ANS: Applying tip should be placed about 1 cm into the nose. Squeeze the recommended number of drops into the nasal opening without touching the sides. Allow the medication to spread throughout the nasal cavity by remaining in place for a few minutes. the right way to store this medication.

 

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