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Nanocarriers to Pharmaceutical Dosage Forms for Drug
PCE401 Assignment 1: Dr. N Ebrahim
Reducing the particle size of an Active Pharmaceutical Ingredient (API) has proven to be an
effective and consistent approach to increasing the bioavailability of insoluble medicines with
poor dissolution rates. The dissolution rate is directly proportional to the surface area, according
to the Noyes Whitney equation. One or more orders of magnitude improvement in dissolution
rate can be accomplished by lowering particle sizes from microns to nanometers and thereby
increasing surface area (Lee, 2003). If medications are reduced to a nanoparticle, they can
provide distinct benefits such as increased blood circulation, higher drug affinity, and greater
therapeutic efficacy. Various pharmaceutical nanosystems, such as polymeric nanoparticles,
dendrimers, magnetic nanoparticles, liposomes, metallic nanoparticles (gold NPs, Silver NPS),
and others, might alter the drug delivery process as well as the overall medical service in order to
achieve maximal drug activity (Shirsath and Goswami, 2019). Carrier-based drug delivery is an
alternate method for increasing medication bioavailability while also protecting drug molecules.
Furthermore, the release profile of encapsulated (biodegradable polymer-coated) medicines is
superior to that of traditional dosage forms. Carrier-based delivery is used to administer
therapeutic drugs to specific areas in a regulated manner or as diagnostic instruments. It also
provides a number of advantages in the diagnosis of chronic disorders and illnesses, thanks to its
site-specific and target-oriented delivery (Shirsath and Goswami, 2019).
The loading of drugs/ composition of the nanoparticulate delivery system is done with a variety
of biodegradable carriers. The drug's carrier should be non-reactive or inert. When a polymer or
carrier interacts with medicine, it reduces the drug's effectiveness or causes an unpleasant
reaction. A good carrier is non-reactive, readily accessible, inexpensive, and capable of targeting
specific organs for optimal effectiveness. The purpose of carriers is to transport a certain amount
of medication to a specific location in the body while also maintaining the drug concentration
and delivering the drug to the targeted tissue in a regulated way. Nanocarriers have a number of
advantages such as improved the solubility of medicine that isn't very soluble (Avramović et al.,
2020). Because of the reduction in size, the surface area increases. Coating the medicine with an
appropriate polymer, masks the bitter taste. Maintains therapeutic drug concentration in the
blood, which improves patient compliance. Reduces the number of times you have to take a
decreases side
Reduces/minimizes dosage and toxicity by protecting the medication from enzymatic
breakdown. Delivers the medicine to the desired location and is suitable for controlled release
(Shirsath and Goswami, 2019).
The following are some examples of carrier-based products:
Niosomes Involveve vesicles generating amphiphile, a nonionic surfactant like Span – 60 that is
generally stabilized with cholesterol, and a little quantity of anionic surfactant like diacetyl
phosphate (Muzzalupo and Mazzotta, 2019). Many pharmacological substances can be delivered
in niosomal form and used to treat a variety of disorders. Targeting bioactive compounds,
immunological uses of niosomes, and use in transdermal dosage forms for transdermal drug
delivery using niosomes are some of its therapeutic applications (Muzzalupo and Mazzotta,
Liposomes Are spherical, colloidal, biodegradable vesicles. Its size ranges from a few
micrometers to tens of micrometers. It consists of a bilayer membrane that encases an aqueous
core. These are vesicles that are engaged in one or more phospholipid bilayers. Because of the
polarity of the liposomal core, polar molecules to be encapsulated are absorbed/dissolved within
the phospholipid bilayer (Shirsath and Goswami, 2019). Lipid soluble molecules are
absorbed/dissolved inside the phospholipid bilayer. Liposomes are significant in improving
medication solubility, bioavailability, targeting particular locations, stability, and sustained
release (Mazdaei and Asare-Addo, 2021).
Nanoparticles (nanospheres/ nanocapsules) are amorphous or crystalline solid-state compounds
with particle sizes ranging from 10 to 200 nanometers (Shirsath and Goswami, 2019). They have
the ability to absorb and/or encapsulate drugs, as well as protect them against chemical and
enzymatic destruction (Shirsath and Goswami, 2019). The NPs can be used to extend the release
of medications and to target specific cancer cells/organs, as well as in gene/peptide delivery
treatment via the pre-oral route. Zhang et al. created MSNs, which are mesoporous silica
nanoparticles that may be used to load pharmaceuticals that are weakly water-soluble. The
telmisartan MSNs improved the dissolution rate and drug loading capacity (Mazdaei and
Asare-Addo, 2021).
Microspheres are biodegradable and the creation of prolonged-release formulations and
medication targeting are two major applications of microspheres. Different biodegradable
polymers were utilized to make the microspheres. They are divided into two categories: Natural
Polymers- are acquired from natural sources such as plants, animals, and marine sources, while
Synthetic Polymers- are obtained through chemical reactions or any synthetic method (ie
biodegradable and nonbiodegradable polymers) (ie proteins and carbohydrates) (Shirsath and
Goswami, 2019).
Dosage forms for drug delivery
Solid dosage forms: Oral controlled drug administration is possible with a variety of new
formulations such as nanoparticles, microspheres, and microcapsules. The major benefit of a new
formulation is orally controlled drug delivery (Shirsath and Goswami, 2019).
In pulmonary delivery aerosols, metered dose inhaler systems (MDIs), powders (dry powder
inhalers, DPIs), and solutions (nebulizers) are all examples of pulmonary delivery systems that
may incorporate nanostructures such as liposomes, micelles, nanoparticles, and dendrimers,
among others (Manivannan and Parthiban, 2010). For the treatment of respiratory disorders,
pulmonary delivery systems are employed. By utilizing the lung's inherent capacity to transport
molecules into the bloodstream, this approach is also employed to provide medications for
systemic circulation. This method of administration has the potential for improved bioavailability
and patient compliance (Bajaj and Desai M,2006). The use of an inhalable dry powder for
antituberculosis administration reduces dosage dumping and reduces the frequency of TB
therapy dosing (Miranda et al, 2018).
The vagina is also an excellent location for local and systemic medication administration. This
method has a number of advantages, including fewer hepatic and gastrointestinal adverse effects
and the ability to treat reproductive organs locally. The vaginally given formulations are mostly
utilized for contraception, infection prevention, AIDS, and other sexually transmitted illnesses.
Nanocarrier-based distribution also has the advantage of being more efficient and causing less
toxicity when administered this way (Shirsath and Goswami, 2019).
Liquid dosage forms: Intranasal dosage forms (nasal drops) employ a variety of new carriers,
including microspheres, nanoemulsions, and nanoparticles. The nanoparticulate approach for the
preparation of intranasal dosage forms for drug delivery has several benefits over the oral route,
including the ability to target individuals with dysphagia, nausea, and vomiting, and the
avoidance of first-pass metabolism (Christrup and Lundorff and Werner, 2009). Gellan gum is a
natural gum that is used to promote mucoadhesive and has been linked to residence duration and
bioavailability (Abbas and Marihal, 2014). For ocular delivery and ophthalmic usage (eye
drops), nanocarrier systems such as nanogel and nanoemulsion are available. Because of the use
of physiologically appropriate lipids, the characteristics of nanocarriers for ocular applications
require fewer regulatory criteria. It has the ability to entrap lipophilic medicines, as well as
protect labile molecules and modulate release behavior (Shirsath and Goswami, 2019).
In conclusion, Nanocarriers will play a significant role in the detection and treatment of
numerous diseases in the coming decade in drug delivery. The key difficulty will be the
development of innovative nanocarriers for biomedical applications, as well as the hurdles to
target medication delivery. The ability to localize tumors and image them will help bring
previously unknown nanocarriers into clinical trials. Future studies could focus on non-toxic,
biocompatible, and biodegradable nanocarriers for stimuli-response medication delivery. This
can help to extend the drug release method and prevent the negative effects of unneeded cell
damage.(Mazdaei and Asare-Addo, 2021). Inorganic nanocarriers have a number of advantages
over organic nanocarriers, including the ability to be easily manufactured and controlled in
nature. Hybrid nanocarriers, composite nanocarriers, and multifunctional inorganic nanocarriers
can improve a single nanocarrier's therapeutic and diagnostic efficacy (Mazdaei and Asare-Addo,
● Avramović, N., Mandić, B., Savić-Radojević, A. and Simić, T. (2020). Polymeric
Nanocarriers of Drug Delivery Systems in Cancer Therapy. Pharmaceutics, 12(4), p.298.
● Mazdaei, M. and Asare-Addo, K. (2021). A mini-review of Nanocarriers in drug delivery
systems Nanocarriers in drug delivery systems. British Journal of Pharmacy.
● Muzzalupo, R. and Mazzotta, E. (2019). Do niosomes have a place in the field of drug
delivery? Expert Opinion on Drug Delivery, 16(11), pp.1145–1147.
● Shirsath, N.R., and Goswami, A.K. (2019). Nanocarriers Based Novel Drug Delivery as
Effective Drug Delivery: A Review. Current Nanomaterials, 4(2), pp.71–83.